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Details

Stereochemistry ABSOLUTE
Molecular Formula C19H18F6N4O3.ClH
Molecular Weight 500.823
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of RETAGLIPTIN HYDROCHLORIDE

SMILES

Cl.COC(=O)C1=C2CN(CCN2C(=N1)C(F)(F)F)C(=O)C[C@H](N)CC3=C(F)C=C(F)C(F)=C3

InChI

InChIKey=DIUZSRUIUOLMSO-HNCPQSOCSA-N
InChI=1S/C19H18F6N4O3.ClH/c1-32-17(31)16-14-8-28(2-3-29(14)18(27-16)19(23,24)25)15(30)6-10(26)4-9-5-12(21)13(22)7-11(9)20;/h5,7,10H,2-4,6,8,26H2,1H3;1H/t10-;/m1./s1

HIDE SMILES / InChI

Molecular Formula C19H18F6N4O3
Molecular Weight 464.3616
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

SP-2086 H3PO4 (Retagliptin Phosphate), tetrahydro-imidazo[1,5-a] pyrazine derivative, is a competitive DPP-4 inhibitor innovated in China under development by Jiangsu Hengrui Medicine for the treatment of Type 2 diabetes. In completed phase II trials, retagliptin monotherapy or in combination with metformin significantly decreased the HbA1c level in type 2 diabetic patients. Two phase III trials for retagliptin monotherapy aCnd in combination with metformin, respectively, were ongoing in China. Jiangsu Hengrui Medicine withdrew its application from the Chinese FDA in April 2016 but is expected to refile the application.

Approval Year

PubMed

PubMed

TitleDatePubMed
An update on DPP-4 inhibitors in the management of type 2 diabetes.
2016 Dec
[Pharmacokinetics of Phosphate Retagliptin Tabletin in Patients with Renal Dysfunction].
2018 Jan

Sample Use Guides

The dosage of phosphate retagliptin tablet is recommended at 100 mg/d for patients with normal renal function and those with mild renal dysfunction,at 50 mg/d for patients with moderate renal dysfunction,and at 25 mg/d for patients with severe renal dysfunction.
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Fri Dec 15 17:18:03 GMT 2023
Edited
by admin
on Fri Dec 15 17:18:03 GMT 2023
Record UNII
7F70K4065S
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
RETAGLIPTIN HYDROCHLORIDE
Common Name English
IMIDAZO(1,5-A)PYRAZINE-1-CARBOXYLIC ACID, 7-((3R)-3-AMINO-1-OXO-4-(2,4,5-TRIFLUOROPHENYL)BUTYL)-5,6,7,8-TETRAHYDRO-3-(TRIFLUOROMETHYL)-, METHYL ESTER, HYDROCHLORIDE (1:1)
Systematic Name English
Code System Code Type Description
CAS
1174038-86-8
Created by admin on Fri Dec 15 17:18:03 GMT 2023 , Edited by admin on Fri Dec 15 17:18:03 GMT 2023
PRIMARY
PUBCHEM
44193829
Created by admin on Fri Dec 15 17:18:03 GMT 2023 , Edited by admin on Fri Dec 15 17:18:03 GMT 2023
PRIMARY
FDA UNII
7F70K4065S
Created by admin on Fri Dec 15 17:18:03 GMT 2023 , Edited by admin on Fri Dec 15 17:18:03 GMT 2023
PRIMARY
Related Record Type Details
ACTIVE MOIETY