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Details

Stereochemistry ABSOLUTE
Molecular Formula C19H18F6N4O3.H3O4P
Molecular Weight 562.3568
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of RETAGLIPTIN PHOSPHATE

SMILES

OP(O)(O)=O.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=SFNHOWDAQMIJPX-HNCPQSOCSA-N
InChI=1S/C19H18F6N4O3.H3O4P/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;1-5(2,3)4/h5,7,10H,2-4,6,8,26H2,1H3;(H3,1,2,3,4)/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 H3O4P
Molecular Weight 97.9952
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 17:26:38 GMT 2023
Edited
by admin
on Fri Dec 15 17:26:38 GMT 2023
Record UNII
24NZ3UE3DJ
Record Status Validated (UNII)
Record Version
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Name Type Language
RETAGLIPTIN PHOSPHATE
Common Name English
SP-2086(H3PO4)
Code 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, PHOSPHATE (1:1)
Common Name English
Code System Code Type Description
PUBCHEM
49820554
Created by admin on Fri Dec 15 17:26:38 GMT 2023 , Edited by admin on Fri Dec 15 17:26:38 GMT 2023
PRIMARY
CAS
1256756-88-3
Created by admin on Fri Dec 15 17:26:38 GMT 2023 , Edited by admin on Fri Dec 15 17:26:38 GMT 2023
PRIMARY
FDA UNII
24NZ3UE3DJ
Created by admin on Fri Dec 15 17:26:38 GMT 2023 , Edited by admin on Fri Dec 15 17:26:38 GMT 2023
PRIMARY
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ACTIVE MOIETY