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A 922500 (CAS 959122-11-3)
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Synonym:
DGAT-1Inhibitor 4a
Application:
A diacyl glycerolacyltransferase 1 inhibitor
CAS Number:
959122-11-3
Purity:
≥96%
Molecular Weight:
428.48
Molecular Formula:
C26H24N2O4
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
* Refer to Certificate of Analysis for lot specific data (including water content).
A 922500 is a diacyl glycerolacyltransferase 1 (DGAT-1) inhibitor (IC50 values are 7 and 24 nM at human and mouse DGAT-1 respectively) that is devoid of activity at DGAT-2, ACAT1 or ACAT2.
References
Zhao et al (2008) Validation of diacyl glycerolacyltransferase I as a novel target of obesity and dyslipidemia using a potent and selective small molecule inhibitor. J.Med.Chem. 51 380. King et al (2009) Diacylglycerol acyltransferase 1 inhibition lowers serum triglycerides in the zucker fatty rat and the hyperlipidemic hamster. J.Pharmacol.Exp.Ther. 330 526.
Physical State
:
Solid
Solubility
:
Soluble in DMSO (50 mM), ethanol (~0.2 mg/ml), DMF (~20 mg/ml), DMSO:PBS (1:10 pH 7.2) (~0.1 mg/ml), and water (<1 mg/ml) at 25° C.
Storage
:
Desiccate at -20° C
Boiling Point
:
576.11° C at 760 mmHg (Predicted)
Density
:
1.32 g/cm3 (Predicted)
Refractive Index
:
n20D 1.68 (Predicted)
IC50
:
DGAT-1: IC50 = 7 nM (human); DGAT-1: IC50 = 24 nM (mouse); DGAT-2: IC50 = 53 µM; acyl coenzyme A cholesterol acyltransferase-1: IC50 = 296 µM; acyl coenzyme A cholesterol acyltransferase-1: IC50 = 296 µM
pK Values
:
pKa: 4.32 (Predicted), pKb: 0.3 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
RTECS
:
GU8624000
PubChem CID
:
24768261
MDL Number
:
MFCD12828780
SMILES
:
O=C(Nc1ccc(cc1)c1ccc(cc1)C(=O)[[email protected]@H]1CCC[[email protected]]1C(=O)O)Nc1ccccc1
Download SDS (MSDS)
Certificate of Analysis
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Rated 5 out of
5
by
HF from
Tsuda et al
Tsuda et al. (PubMed ID 25405858) found that A- 922500 attenuated obesity and insulin resistance without causing skin problems in mice via DGAT1 inhibition. -SCBT Publication Review
Date published: 2015-04-29
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