Details
Stereochemistry | ACHIRAL |
Molecular Formula | C27H30N7OS.K.3H2O |
Molecular Weight | 593.783 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O.O.O.[K+].CCCCC1=NC(C)=C(CC(=S)N(C)C)C(=O)N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NN=N[N-]4
InChI
InChIKey=IJEKJHQBGZFMMI-UHFFFAOYSA-N
InChI=1S/C27H30N7OS.K.3H2O/c1-5-6-11-24-28-18(2)23(16-25(36)33(3)4)27(35)34(24)17-19-12-14-20(15-13-19)21-9-7-8-10-22(21)26-29-31-32-30-26;;;;/h7-10,12-15H,5-6,11,16-17H2,1-4H3;;3*1H2/q-1;+1;;;
Molecular Formula | H2O |
Molecular Weight | 18.0153 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C27H31N7OS |
Molecular Weight | 501.646 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | K |
Molecular Weight | 39.0983 |
Charge | 1 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/22864732Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/23811571, http://www.boryung.co.kr/eng/product/mainProduct.do
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22864732
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/23811571, http://www.boryung.co.kr/eng/product/mainProduct.do
Fimasartan is a angiotensin II receptor antagonist which was developed in Korea for the treatment of hypertension. The drug is available in different forms: Kanarb, Dukarb (in combination with Amlodipine), Tuvero (in combination with Rosuvastatin). Fimasartan was tested to be effective in Mexican and Russian population and now is being tested in the USA.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2094256 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23811571 |
0.13 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | KANARB Approved UseFor the treatment of essential hypertension. Launch Date1.28329921E12 |
PubMed
Title | Date | PubMed |
---|---|---|
Fimasartan, anti-hypertension drug, suppressed inducible nitric oxide synthase expressions via nuclear factor-kappa B and activator protein-1 inactivation. | 2013 |
|
Influence of Fimasartan (a Novel AT(1) Receptor Blocker) on Catecholamine Release in the Adrenal Medulla of Spontaneously Hypertensive Rats. | 2013 Feb |
|
Effect of renal function on the pharmacokinetics of fimasartan: a single-dose, open-label, Phase I study. | 2014 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26272450
Fimasartan is taken as a single oral dose of 60-mg tablet or a single 30-mg intravenous (IV) infusion.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23811571
Rabbit thoracic aorta cells were incubated with different concentrations of fimasartan ((0.1, 1, 10 nM). At those concentrations fimasartan caused nonparallel rightward shifts in the concentration–contractile response curve to Ang II with a significant reduction in the maximal contractile response to 96.6, 47 and 18%, respectively.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 08:10:40 UTC 2023
by
admin
on
Sat Dec 16 08:10:40 UTC 2023
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Record UNII |
4516BN0T4B
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Record Status |
Validated (UNII)
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Record Version |
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46929800
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1020110-23-9
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100000165808
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4516BN0T4B
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SUB179690
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PARENT -> SALT/SOLVATE |
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ANHYDROUS->SOLVATE |
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ACTIVE MOIETY |