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

CAS: 959122-11-3 Cat. No.: A408455 분자식: C₂₆H₂₄N₂O₄ 분자량: 428.48 EC 번호: 688-540-9

등급 & 순도 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

개요

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%

사양

동의어

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

사양 및 순도

10mM in DMSO

생화학 및 생리적 메커니즘

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.

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

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작업 유형

INHIBITOR

이름과 식별자

이성체 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

분자량

428.48

Reaxy-Rn

29788907

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=29788907&ln=

관련 대상(인간)

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)

화학 및 물리적 특성

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