DGAT-1 inhibitor

DGAT-1 inhibitor Basic information
Product Name:DGAT-1 inhibitor
Synonyms:(1R,2R)-2-[[4'-[[(Phenylamino)carbonyl]amino][1,1'-biphenyl]-4-yl]carbonyl]cyclopentanecarboxylic acid;DGAT-1 inhibitor;Diacyl glycerolacyltransferase 1 inhibitor;A922500;A922500(DGAT-1 Inhibitor 4a);enylureido)biphenyl(1R,2R)-2-(4'-(3-phcarbonyl)cyclopentanecarboxylic acid;DGAT-1 Inhibitor 4a;(1R,2R)-2-(4'-(3-phenylureido)biphenylcarbonyl)cyclopentanecarboxylic acid
CAS:959122-11-3
MF:C26H24N2O4
MW:428.48
EINECS:
Product Categories:Inhibitor;Inhibitors;APIs
Mol File:959122-11-3.mol
DGAT-1 inhibitor Structure
DGAT-1 inhibitor Chemical Properties
density 1.323
storage temp. -20°C
solubility ≥21.25 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
form Light yellow solid
Safety Information
Hazard Codes T,N
Risk Statements 25-36-50
Safety Statements 26-45-61
RIDADR UN 2811 6.1 / PGIII
WGK Germany 3
MSDS Information
DGAT-1 inhibitor Usage And Synthesis
UsesA922500 has been used in the inhibition of diacylglycerol acyltransferase (DGAT) in epithelial human breast cancer cell line (MDA-MB-231), digitonin-permeabilized human cancer cells, human myotubes and macrophages.
DefinitionChEBI: A 922500 is an aromatic ketone.
Biological ActivityDiacylglycerol acyltransferase 1 (DGAT-1) inhibitor (IC 50 values are 7 and 24 nM at human and mouse DGAT-1 respectively) that is devoid of activity at DGAT-2, ACAT1 or ACAT2. Induces significant weight loss without altering food intake, and decreases liver and plasma triglyceride levels in vivo . Orally active.
Biochem/physiol ActionsThe diacylglycerol acyltransferase (DGAT) 1 inhibitor A922500 was shown to effectively reduce postprandial serum triglyceride levels in rodents at concentrations of 0.03, 0.3 and 3 mg/kg. These results suggest A922500 may have beneficial effects in reducing the risk of cardiovascular disease.
DGAT-1 inhibitor Preparation Products And Raw materials
Tofacitinib NS-398 Urease inhibitor SGX-523 GSK256066 (1R,2R)-1-(tert-butoxycarbonylamino)-2-(difluoromethyl)cyclopropanecarboxylic acid Quizartinib (AC220) PF-562271 Selumetinib

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