RANOLAZINE

Details

Stereochemistry	RACEMIC
Molecular Formula	C24H33N3O4
Molecular Weight	427.5374
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cc1cccc(C)c1N=C(CN2CCN(CC2)CC(COc3ccccc3OC)O)O

InChI

InChIKey=XKLMZUWKNUAPSZ-UHFFFAOYSA-N

InChI=1S/C24H33N3O4/c1-18-7-6-8-19(2)24(18)25-23(29)16-27-13-11-26(12-14-27)15-20(28)17-31-22-10-5-4-9-21(22)30-3/h4-10,20,28H,11-17H2,1-3H3,(H,25,29)

HIDE SMILES / InChI

Molecular Formula	C24H33N3O4
Molecular Weight	427.5374
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021526s000lbl.pdf
Curator's Comment:: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/16196483

Ranolazine is a metabolic modulator developed by Syntex (Roche) and sold under the trade name Ranexa by Gilead Sciences. Ranexa has antianginal and anti-ischemic effects that do not depend upon reductions in heart rate or blood pressure. The mechanism of action of ranolazine is unknown. It does not increase the rate-pressure product, a measure of myocardial work, at maximal exercise. In vitro studies suggest that ranolazine is a P-gp inhibitor. Ranolazine is believed to have its effects via altering the trans-cellular late sodium current. It is by altering the intracellular sodium level that ranolazine affects the sodium-dependent calcium channels during myocardial ischemia. Thus, ranolazine indirectly prevents the calcium overload that causes cardiac ischemia. Because Ranexa prolongs the QT interval, it should be reserved for patients who have not achieved an adequate response with other antianginal drugs. Ranexa should be used in combination with amlodipine, beta-blockers or nitrates. The effect on angina rate or exercise tolerance appeared to be smaller in women than men.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Sodium channel protein type V alpha subunit 47 Target ID: CHEMBL1980 Sources: https://www.ncbi.nlm.nih.gov/pubmed/?term=18462746	Inhibitor 7728

Conditions

Condition	Modality	Targets	Highest Phase	Product
Angina 15 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021526s000lbl.pdf	Primary		Approved 8043	RANEXA Approved Use Ranexa is indicated for the treatment of chronic angina. Ranexa may be used with beta-blockers, nitrates, calcium channel blockers, anti-platelet therapy, lipid-lowering therapy, ACE inhibitors, and angiotensin receptor blockers. Ranexa is indicated for the treatment of chronic angina. (1) Launch Date 1.13831995E12

C_max

Value	Dose	Co-administered	Analyte	Population
741.5 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/23355361	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:		RANOLAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2600 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021526s028lbl.pdf	1000 mg 2 times / day steady-state, oral dose: 1000 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		RANOLAZINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
9862.7 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/23355361	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:		RANOLAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Co-administered	Analyte	Population
6.4 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/23355361	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:		RANOLAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021526s028lbl.pdf	1000 mg 2 times / day steady-state, oral dose: 1000 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		RANOLAZINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
38% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021526s028lbl.pdf	1000 mg 2 times / day steady-state, oral dose: 1000 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		RANOLAZINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
2000 mg single, oral Highest studied dose Dose: 2000 mg Route: oral Route: single Dose: 2000 mg Sources: https://pubmed.ncbi.nlm.nih.gov/19763194/	unhealthy, 57-83 years n = 18 Health Status: unhealthy Condition: Atrial fibrillation Age Group: 57-83 years Sex: M+F Population Size: 18 Sources: https://pubmed.ncbi.nlm.nih.gov/19763194/	Sources: https://pubmed.ncbi.nlm.nih.gov/19763194/
1500 mg 2 times / day steady, oral Highest studied dose Dose: 1500 mg, 2 times / day Route: oral Route: steady Dose: 1500 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15093870	unhealthy, 64.3 years (range: 39–85 years) n = 60 Health Status: unhealthy Condition: Stable Angina Age Group: 64.3 years (range: 39–85 years) Sex: M+F Population Size: 60 Sources: https://pubmed.ncbi.nlm.nih.gov/15093870	Other AEs: Dizziness, Nausea... Other AEs: Dizziness (12.3%) Nausea (8.6%) Asthenia (6.4%) Constipation (4.3%) Angina pectoris (3.2%) Headache (2.7%) Sweating (2.7%) Sources: https://pubmed.ncbi.nlm.nih.gov/15093870
50 g single, oral Overdose Dose: 50 g Route: oral Route: single Dose: 50 g Co-administed with:: quetiapine(therapeutic or subtherapeutic) valproate(therapeutic or subtherapeutic) mirtazapine(therapeutic or subtherapeutic) Sources: https://pubmed.ncbi.nlm.nih.gov/31119956	unhealthy, 65 years n = 1 Health Status: unhealthy Age Group: 65 years Sex: F Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/31119956	Other AEs: Electrocardiogram QTc interval prolonged... Other AEs: Electrocardiogram QTc interval prolonged (grade 5) Sources: https://pubmed.ncbi.nlm.nih.gov/31119956
1000 mg 2 times / day steady, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: steady Dose: 1000 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021526s000lbl.pdf	unhealthy, adult n = 835 Health Status: unhealthy Condition: chronic angina Age Group: adult Population Size: 835 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021526s000lbl.pdf	Disc. AE: Dizziness, Nausea... AEs leading to discontinuation/dose reduction: Dizziness (1.3%) Nausea (1%) Asthenia (0.5%) Constipation (0.5%) Headache (0.5%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021526s000lbl.pdf

AEs

AE	Significance	Dose	Population
Dizziness	12.3%	1500 mg 2 times / day steady, oral Highest studied dose Dose: 1500 mg, 2 times / day Route: oral Route: steady Dose: 1500 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15093870	unhealthy, 64.3 years (range: 39–85 years) n = 60 Health Status: unhealthy Condition: Stable Angina Age Group: 64.3 years (range: 39–85 years) Sex: M+F Population Size: 60 Sources: https://pubmed.ncbi.nlm.nih.gov/15093870
Headache	2.7%	1500 mg 2 times / day steady, oral Highest studied dose Dose: 1500 mg, 2 times / day Route: oral Route: steady Dose: 1500 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15093870	unhealthy, 64.3 years (range: 39–85 years) n = 60 Health Status: unhealthy Condition: Stable Angina Age Group: 64.3 years (range: 39–85 years) Sex: M+F Population Size: 60 Sources: https://pubmed.ncbi.nlm.nih.gov/15093870
Sweating	2.7%	1500 mg 2 times / day steady, oral Highest studied dose Dose: 1500 mg, 2 times / day Route: oral Route: steady Dose: 1500 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15093870	unhealthy, 64.3 years (range: 39–85 years) n = 60 Health Status: unhealthy Condition: Stable Angina Age Group: 64.3 years (range: 39–85 years) Sex: M+F Population Size: 60 Sources: https://pubmed.ncbi.nlm.nih.gov/15093870
Angina pectoris	3.2%	1500 mg 2 times / day steady, oral Highest studied dose Dose: 1500 mg, 2 times / day Route: oral Route: steady Dose: 1500 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15093870	unhealthy, 64.3 years (range: 39–85 years) n = 60 Health Status: unhealthy Condition: Stable Angina Age Group: 64.3 years (range: 39–85 years) Sex: M+F Population Size: 60 Sources: https://pubmed.ncbi.nlm.nih.gov/15093870
Constipation	4.3%	1500 mg 2 times / day steady, oral Highest studied dose Dose: 1500 mg, 2 times / day Route: oral Route: steady Dose: 1500 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15093870	unhealthy, 64.3 years (range: 39–85 years) n = 60 Health Status: unhealthy Condition: Stable Angina Age Group: 64.3 years (range: 39–85 years) Sex: M+F Population Size: 60 Sources: https://pubmed.ncbi.nlm.nih.gov/15093870
Asthenia	6.4%	1500 mg 2 times / day steady, oral Highest studied dose Dose: 1500 mg, 2 times / day Route: oral Route: steady Dose: 1500 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15093870	unhealthy, 64.3 years (range: 39–85 years) n = 60 Health Status: unhealthy Condition: Stable Angina Age Group: 64.3 years (range: 39–85 years) Sex: M+F Population Size: 60 Sources: https://pubmed.ncbi.nlm.nih.gov/15093870
Nausea	8.6%	1500 mg 2 times / day steady, oral Highest studied dose Dose: 1500 mg, 2 times / day Route: oral Route: steady Dose: 1500 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15093870	unhealthy, 64.3 years (range: 39–85 years) n = 60 Health Status: unhealthy Condition: Stable Angina Age Group: 64.3 years (range: 39–85 years) Sex: M+F Population Size: 60 Sources: https://pubmed.ncbi.nlm.nih.gov/15093870
Electrocardiogram QTc interval prolonged	grade 5	50 g single, oral Overdose Dose: 50 g Route: oral Route: single Dose: 50 g Co-administed with:: quetiapine(therapeutic or subtherapeutic) valproate(therapeutic or subtherapeutic) mirtazapine(therapeutic or subtherapeutic) Sources: https://pubmed.ncbi.nlm.nih.gov/31119956	unhealthy, 65 years n = 1 Health Status: unhealthy Age Group: 65 years Sex: F Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/31119956
Asthenia	0.5% Disc. AE	1000 mg 2 times / day steady, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: steady Dose: 1000 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021526s000lbl.pdf	unhealthy, adult n = 835 Health Status: unhealthy Condition: chronic angina Age Group: adult Population Size: 835 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021526s000lbl.pdf
Constipation	0.5% Disc. AE	1000 mg 2 times / day steady, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: steady Dose: 1000 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021526s000lbl.pdf	unhealthy, adult n = 835 Health Status: unhealthy Condition: chronic angina Age Group: adult Population Size: 835 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021526s000lbl.pdf
Headache	0.5% Disc. AE	1000 mg 2 times / day steady, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: steady Dose: 1000 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021526s000lbl.pdf	unhealthy, adult n = 835 Health Status: unhealthy Condition: chronic angina Age Group: adult Population Size: 835 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021526s000lbl.pdf
Nausea	1% Disc. AE	1000 mg 2 times / day steady, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: steady Dose: 1000 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021526s000lbl.pdf	unhealthy, adult n = 835 Health Status: unhealthy Condition: chronic angina Age Group: adult Population Size: 835 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021526s000lbl.pdf
Dizziness	1.3% Disc. AE	1000 mg 2 times / day steady, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: steady Dose: 1000 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021526s000lbl.pdf	unhealthy, adult n = 835 Health Status: unhealthy Condition: chronic angina Age Group: adult Population Size: 835 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021526s000lbl.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1601 inhibitor 1467		substrate 1118 inhibitor 1702	inhibitor 1475

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1330 OCT2 594 CYP2C8 818	P-gp 1400

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP2D6 1738	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021526s035lbl.pdf Page: 12, 13	moderate
CYP2C8 865	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/021526Orig1s004ClinPharmR.pdf Page: 5, 87	no
P-gp 1514	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021526_s000_Ranexa_BioPharmr.pdf Page: 97, 145	yes [Ki 197 uM]	yes (co-administration study) Comment: ketoconazole, diltiazem and verapamil increase the exposure to ranolazine by a factor of 2.0 or more and the impact on the PK of ranolazine is clinically significant Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021526_s000_Ranexa_BioPharmr.pdf Page: 97, 145
CYP3A4 1772	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021526_s000_Ranexa_BioPharmr.pdf Page: 121, 315	yes
OCT2 595	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021526s035lbl.pdf Page: 12, 13	yes

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A4 1601	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021526_s000_Ranexa_BioPharmr.pdf Page: 96, 131	major	yes (co-administration study) Comment: ketoconazole, diltiazem and verapamil increase the exposure to ranolazine by a factor of 2.0 or more and the impact on the PK of ranolazine is clinically significant Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021526_s000_Ranexa_BioPharmr.pdf Page: 96, 131
CYP2D6 1118	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021526_s000_Ranexa_BioPharmr.pdf Page: 96, 131	minor	yes (co-administration study) Comment: paroxetine increased the exposure of ranolazine by <20% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021526_s000_Ranexa_BioPharmr.pdf Page: 96, 131
P-gp 1400	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021526_s000_Ranexa_BioPharmr.pdf Page: 97, 144	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1507	inhibitor 1489 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021526_s000_Ranexa_Pharmr.pdf Page: 102.0

Sourcing

Vendor/Aggregator	ID	URL
3B Scientific (Wuhan) Corp	3B2-0643	http://www.3bsc.com/index/pro_info.php?id=19999
AA Blocks	AA00H8NU	http://www.aablocks.com/goods/Goods/detail?id=AA00H8NU
AEchem Scientific Corp., USA	AE1-016762	http://www.aechemsc.com/info_products/AE1-016762.php
AHH Chemical co.,ltd	API-1613	http://www.ahhchemical.com/product/API-1613.html
AHH Chemical co.,ltd	MT-01113	http://www.ahhchemical.com/product/MT-01113.html
AHH Chemical co.,ltd	MT-01114	http://www.ahhchemical.com/product/MT-01114.html
AK Scientific, Inc. (AKSCI)	H959	http://www.aksci.com/item_detail.php?cat=H959
Aaron Chemicals	AR00H9FM	http://www.aaronchem.com/95635-55-5
AbMole Bioscience	M3956	http://www.abmole.com/products/ranolazine-dihydrochloride.html
AbMole Bioscience	M5922	http://www.abmole.com/products/ranolazine.html
Acadechem	ACDS-070678	http://www.acadechemical.com/product/145377
Achemo Scientific Limited	AC-15291	http://www.achemo.com/search/?Keyword= 95635-55-5
Achemtek	0102-032078	http://www.achemtek.com/95635-55-5
Alfa Chemistry	AP95635555	https://reagents.alfa-chemistry.com/product/ranolazine-cas-95635-55-5-18942.html
Alfa Chemistry	1054624-77-9	https://www.alfa-chemistry.com/cas_1054624-77-9.htm
Angene	AGN-PC-0WAE7I	http://www.angenechemical.com/productshow/AGN-PC-0WAE7I.html
Ark Pharm	AK-72950	http://www.arkpharminc.com/products/95635-55-5.html
AstaTech, Inc.	23746	http://www.astatechinc.com/CPSResult.php?CRNO=27415
Aurum Pharmatech LLC	S-1794	http://www.Aurumpharmatech.com/Product/ProductDetails/S_1794
AvaChem Scientific	2451B	http://www.avachem.com/productSearch.asp?2451B
Avantor Inc	BT224750-1G	https://us.vwr.com/store/product/16640415/ranolazine
Avantor Inc	BT224750-5G	https://us.vwr.com/store/product/16640415/ranolazine
BLD Pharm	BD23248	http://www.bldpharm.com/products/95635-55-5.html
BOC Sciences	1092804-87-9	https://www.bocsci.com/ranolazine-d5-cas-1092804-87-9-item-483673.html
BOC Sciences	1092804-88-0	https://www.bocsci.com/ranolazine-d8-cas-1092804-88-0-item-482712.html
BioChemPartner	BCP04190	http://www.biochempartner.com/95635-55-5-BCP04190
BioCrick	BCC3847	http://www.biocrick.com/Ranolazine-BCC3847.html
Boerchem	BC205445	http://www.boerchem.com/?product_34594.html
CSNpharm	CSN13104	https://www.csnpharm.com/products/ranolazine.html
Chem Scene	CS-2292	http://www.chemscene.com/95635-55-5.html
ChemMol	30102623	http://www.chemmol.com/chemmol/30102623.html
ChemMol	30107388	http://www.chemmol.com/chemmol/30107388.html
ChemMol	44002143	http://www.chemmol.com/chemmol/44002143.html
ChemMol	49400256	http://www.chemmol.com/chemmol/49400256.html
ChemMol	81411415	http://www.chemmol.com/chemmol/81411415.html
ChemReagents	80017137	http://www.chemreagents.com/Product/Product.asp?ProductID=80017137
Chemenu	CM110525	http://www.chemenu.com/products/CM110525
Chemspace	CSSB00000695080	https://chem-space.com/CSSB00000695080
Clearsynth	CS-T-41527	https://www.clearsynth.com/en/CST41527.html
DC Chemicals	DCAPI1391	http://www.dcchemicals.com//product_show-Ranolazine_Ranexa_.html
Enamine	Z68563450	https://www.enaminestore.com/catalog/Z68563450
Finetech	FT-0674327	http://www.finetechnology-ind.com/prod/detail/pub/1054624-77-9.html
Finetech	FT-0601594	http://www.finetechnology-ind.com/prod/detail/pub/95635-55-5.html
Glentham Life Sciences	GP0528	http://www.glentham.com/products/product/GP0528/
LGC Standards	MM3496.00	https://www.lgcstandards.com/US/en/p/MM3496.00
Lab Network	LN00176820	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN00176820
Matrix Scientific	76093	https://www.matrixscientific.com/076093.html
MedChem Express	HY-B0280	https://www.medchemexpress.com/ranolazine.html
MuseChem	A000721	https://www.musechem.com/product/A000721.html
MuseChem	M094380	https://www.musechem.com/product/M094380.html
OChem	5051	http://www.ocheminc.com/index.php?act=psearch&pid=635R555
Oakwood	79440	http://www.oakwoodchemical.com/ProductsList.aspx?CategoryID=-2&txtSearch=64614&ExtHyperLink=1
Parchem	45709	https://www.parchem.com/chemical-supplier-distributor/N-(2-6-Dimethylphenyl)-2-(4-(2-hydroxy-3-(2-methoxyphenoxy)propyl)piperazin-1-yl)acetamide-045709.aspx
Selleck Chemicals	S1799	http://www.selleckchem.com/products/Ranolazine(Ranexa).html
Sinfoo Biotech	S055021	http://www.sinfoobiotech.com/product/1058419
Smolecule	S572521	https://www.smolecule.com/products/s572521
Synblock Inc	SB13209	http://www.synblock.com/product/95635-55-5.html
Synblock Inc	PB21724	http://www.synblock.com/product/95635-56-6.html
THE BioTek	bt-460990	https://www.thebiotek.com/product/others/bt-460990
TripleBond	CR0012	http://www.triplebond-canada.com/prod/1553/
VladaChem	VL144119	https://www.vladachem.com/product.php?products=95635-55-5
Yuhao Chemical	LL1863	http://www.chemyuhao.com/110445-25-5.html
Yuhao Chemical	RT10121	http://www.chemyuhao.com/95635-55-5.html
abcr GmbH	AB439887	http://www.abcr.com/shop/en/AB439887
eNovation Chemicals	D510796	https://www.enovationchem.com/ProductDetails.asp?ProductID=D510796
eNovation Chemicals	D960655	https://www.enovationchem.com/ProductDetails.asp?ProductID=D960655
iChemical	EBD17867	http://www.ichemical.com/chemicals/cas-95635-55-5
iChemical	EBD84673	http://www.ichemical.com/products/142387-99-3.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
mcule	MCULE-8182023610	https://mcule.com/MCULE-8182023610/

PubMed

Title	Date	PubMed
Effects of ranolazine with atenolol, amlodipine, or diltiazem on exercise tolerance and angina frequency in patients with severe chronic angina: a randomized controlled trial.	2004 Jan 21	14734593
Ranolazine, an inhibitor of the late sodium channel current, reduces postischemic myocardial dysfunction in the rabbit.	2006 Dec	17220471
Effects of ranolazine on recurrent cardiovascular events in patients with non-ST-elevation acute coronary syndromes: the MERLIN-TIMI 36 randomized trial.	2007 Apr 25	17456819
Ranolazine block of human Na v 1.4 sodium channels and paramyotonia congenita mutants.	2011 Mar-Apr	21317558

Patents

Sample Use Guides

In Vivo Use Guide

Dosing should be initiated at 500 mg b.i.d. and increased to 1000 mg b.i.d., as needed, based on clinical symptoms. The maximum recommended daily dose is 1000 mg b.i.d.

Route of Administration: Oral

In Vitro Use Guide

Ranolazine (Rn) acts in the central nervous system and it has been proposed for the treatment of pain and epileptic disorders. Under the hypothesis that ranolazine could act as a neuroprotective drug, was studied its effects on astrocytes and neurons in primary culture. It was incubated rat astrocytes and neurons in primary cultures for 24 hours with Rn (10-7, 10-6 and 10-5 M). Cell viability and proliferation were measured using trypan blue exclusion assay, MTT conversion assay and LDH release assay. Apoptosis was determined by Caspase 3 activity assay. The effects of Rn on pro-inflammatory mediators IL-β and TNF-α was determined by ELISA technique, and protein expression levels of Smac/Diablo, PPAR-γ, Mn-SOD and Cu/Zn-SOD by western blot technique. Rn could act as a neuroprotective drug in the central nervous system by promoting astrocyte viability, preventing necrosis and apoptosis, inhibiting inflammatory phenomena and inducing anti-inflammatory and antioxidant agents.

Substance Class	Chemical Created by `admin` on `Fri Jun 25 21:34:45 UTC 2021` Edited by `admin` on `Fri Jun 25 21:34:45 UTC 2021`
Record UNII	A6IEZ5M406
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

RANOLAZINE

Official Name

English

RANOLAZINE [USP-RS]

Common Name

English

CVT-303

Code

English

RAN D

Common Name

English

RAN4

Common Name

English

RANEXA

Brand Name

English

(+/-)-N-(2,6-DIMETHYLPHENYL)-4-(2-HYDROXY-3-(2-METHOXYPHENOXY)PROPYL)-1-PIPERAZINEACETAMIDE

Systematic Name

English

1-PIPERAZINEACETAMIDE, N-(2,6-DIMETHYLPHENYL)-4-(2-HYDROXY-3-(2-METHOXYPHENOXY)PROPYL)-, (+/-)

Common Name

English

RANOLAZINE [WHO-DD]

Common Name

English

RANOLAZINE [EMA EPAR]

Common Name

English

NSC-759100

Code

English

N-(2,6-DIMETHYLPHENYL)-2-(4-((2RS)-2-HYDROXY-3-(2-METHOXYPHENOXY)PROPYL)PIPERAZIN-1-YL)ACETAMIDE

Systematic Name

English

1-PIPERAZINEACETAMIDE, N-(2,6-DIMETHYLPHENYL)-4-(2-HYDROXY-3-(2-METHOXYPHENOXY)PROPYL)-

Systematic Name

English

RS-43285-003

Code

English

RANOLAZINE [VANDF]

Common Name

English

RANOLAZINE [USAN]

Common Name

English

RANOLAZINE [ORANGE BOOK]

Common Name

English

RANOLAZINE [INN]

Common Name

English

RANOLAZINE [MART.]

Common Name

English

RANOLAZINE [MI]

Common Name

English

Classification Tree Code System Code

LIVERTOX

834