Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C36H29FN2O4 |
| Molecular Weight | 572.6249 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)[C@H](CC1=CC=C(OCCN2C3=C(C=CC=C3)C4=C2C=CC=C4)C=C1)NC5=C(C=CC=C5)C(=O)C6=CC=C(F)C=C6
InChI
InChIKey=QNLWMPLUWMWDMQ-YTTGMZPUSA-N
InChI=1S/C36H29FN2O4/c37-26-17-15-25(16-18-26)35(40)30-9-1-4-10-31(30)38-32(36(41)42)23-24-13-19-27(20-14-24)43-22-21-39-33-11-5-2-7-28(33)29-8-3-6-12-34(29)39/h1-20,32,38H,21-23H2,(H,41,42)/t32-/m0/s1
| Molecular Formula | C36H29FN2O4 |
| Molecular Weight | 572.6249 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 12:12:54 UTC 2023
by
admin
on
Sat Dec 16 12:12:54 UTC 2023
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| Record UNII |
E6EJV1J6Y0
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| Record Status |
Validated (UNII)
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| Record Version |
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71402018
Created by
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E6EJV1J6Y0
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DTXSID00225352
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743438-45-1
Created by
admin on Sat Dec 16 12:12:54 UTC 2023 , Edited by admin on Sat Dec 16 12:12:54 UTC 2023
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ACTIVE MOIETY |
Class: Anti-hyper-glycaemic, Carbazole, Propionic acid, Small molecule; Mechanism of Action: Peroxisome proliferator-activated receptor alpha agonist, Peroxisome proliferator-activated receptor delta agonist, Peroxisome proliferator-activated receptor gamma agonist; Highest Development Phases: Phase III Type 2 diabetes mellitus, Preclinical for Parkinson's disease; Most Recent Events: 01 Jun 2014 Chipscreen Biosciences initiates enrolment in the phase III CMAS trial for Type-2 diabetes mellitus in China (NCT02173457), 01 May 2014 Phase-III clinical trials in Type-2 diabetes mellitus in China (PO), 29 Apr 2014 Preclinical trials in Parkinson's disease in China (PO)
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ACTIVE MOIETY |
Chiglitazar (CS038), a new chemical entity as a PPAR pan-agonist developed by Chipscreen Bio sciences Ltd., has completed a multi-centered phase IIa trial recently. Chiglitazar , administered for 12 weeks, showed the effects dose-dependently on lowering fasting and postprandial blood glucose, and HbA1C in type 2 diabetes patients. It also lowered the fasting and postprandial serum insulin, and improved lipid profiles. No obvious drug related side effects were observed in the trial. Further clinical studies are under design.
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ACTIVE MOIETY |
Chiglitazar had high distribution in liver, pancreas, and skeleton muscles but was less present in kidney, heart, and adipose in rats. Heart weight increase was not observed in rats treated with chiglitazar for 6 months at a dose as high as 45mg kg1. The in vitro and in vivo differential features of chiglitazar are informative and encouraging for the further development of this synthetic ligand for the potential use in T2DM.
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