A 922500 (CAS 959122-11-3)

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Alternate Names: DGAT-1Inhibitor 4a

Application: A 922500 is a DGAT-1 (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.

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

* Refer to Certificate of Analysis for lot specific data (including water content).

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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 :

n²⁰_D 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 :

pK_a: 4.32 (Predicted), pK_b: 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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A 922500 (CAS 959122-11-3) Product Citations

See how others have used A 922500 (CAS 959122-11-3). Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 22365411 Kim, Y. et al. 2012. Eur J Med Chem. 50: 311-8.

PMID: # 30161232 PLoS Pathog. e1007223.

Citations 1 to 2 of 2 total

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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