A922500 - 10mM in DMSO , CAS No.959122-11-3

CAS: 959122-11-3 Cat. No.: A408455 Formula: C₂₆H₂₄N₂O₄ Molecular Weight: 428.48 EC Number: 688-540-9

GRADE & PURITY 10mM in DMSO

Synonyms

DGAT-1 Inhibitor 4a | Cyclopentanecarboxylic acid, 2-[[4'-[[(phenylamino)carbonyl]amino][1,1'-biphenyl]-4-yl]carbonyl]-, (1R,2R)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

A922500 A922500 (DGAT-1 Inhibitor 4a) is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets.
In vitro

A 922500 inhibits the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 with IC50 of 296 μM. A 922500 potently inhibits huDGAT-1 and mseDGAT-1.

In vivo

Zucker fatty rats and diet-induced dyslipidemic hamsters are dosed orally with A 922500 (0.03, 0.3, and 3 mg/kg) for 14 days. Serum triglycerides ae significantly reduced by the 3 mg/kg dose of A 922500 in both the Zucker fatty rat (39%) and hyperlipidemic hamster (53%). These serum triglyceride changes are accompanied by significant reductions in free fatty acid levels by 32% in the Zucker fatty rat and 55% in the hyperlipidemic hamster. In addition, high-density lipoprotein-cholesterol is significantly increases (25%) in the Zucker fatty rat by A 922500 administered at 3 mg/kg. A 922500 confers weight loss and a reduction in liver triglycerides when dosed chronically in DIO mice and depletes serum triglycerides following a lipid challenge in a dose-dependent manner, thus, reproducing major phenotypical characteristics of DGAT-1(-/-) mice. A 922500 (0.03, 0.3 and 3 mg/kg, p.o.) dose-dependently attenuates the maximal postprandial rise in serum triglyceride concentrations.
Cell Data

cell lines：HUVECs

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

DGAT-1 Inhibitor 4a | Cyclopentanecarboxylic acid, 2-[[4'-[[(phenylamino)carbonyl]amino][1,1'-biphenyl]-4-yl]carbonyl]-, (1R,2R)-

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

A922500 (DGAT-1 Inhibitor 4a) is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Names and Identifiers

• Isomeric SMILES: C1C[C@H]([C@@H](C1)C(=O)O)C(=O)C2=CC=C(C=C2)C3=CC=C(C=C3)NC(=O)NC4=CC=CC=C4
• Molecular Weight: 428.48
• Reaxy-Rn: 29788907
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=29788907&ln=

Associated Targets(Human)

DGAT1 Tclin Diacylglycerol O-acyltransferase 1 (4 Activities)

Discover Target: DGAT1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 15 mg/mL (18.96 mM); Water: Insoluble; Ethanol: Insoluble

References

1. Min Zhou, Xiaojing Zhao, Zixuan Yang, Lihui Meng, Zhaozhe Xin, Sijia Xue, Jinyong Zhang.  (2026)  Ameson portunus ACSL mediates host fatty acid acquisition for intracellular proliferation.  Water Biology and Security,      [PMID:] [10.1016/j.watbs.2026.100699]