A diacylglycerol acyltransferase 1 inhibitor
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A-922500

Item No. 10012708

Technical Information
Formal Name
2R-[[4’-[[(phenylamino)carbonyl]amino][1R,1’-biphenyl]-4-yl-carbonyl]-cyclopentanecarboxylic acid
CAS Number
959122-11-3
Synonyms
  • (1R,2R)-2-(4'-(3-phenylureido)biphenylcarbonyl)-cyclopentanecarboxylic acid
Molecular Formula
C26H24N2O4
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:10): 0.1 mg/mlEthanol: 0.2 mg/ml
SMILES
O=C(NC1=CC=C(C2=CC=C(C([C@@H]3CCC[C@H]3C(O)=O)=O)C=C2)C=C1)NC4=CC=CC=C4
InChi Code
InChI=1S/C26H24N2O4/c29-24(22-7-4-8-23(22)25(30)31)19-11-9-17(10-12-19)18-13-15-21(16-14-18)28-26(32)27-20-5-2-1-3-6-20/h1-3,5-6,9-16,22-23H,4,7-8H2,(H,30,31)(H2,27,28,32)/t22-,23-/m1/s1
InChi Key
BOZRFEQDOFSZBV-DHIUTWEWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    A-922500 is a potent orally active inhibitor of DGAT-1 activity, inhibiting both human and mouse forms of the enzymes with IC50 values of 7 and 24 nM, respectively.1 When administered at 3 mg/kg to DIO mice, A-922500 conferred significant weight loss within seven days without affecting food intake and significantly reduced plasma and liver triglycerides with chronic dosing.1 A-922500 does not inhibit DGAT-2, ACAT-1, or ACAT-2.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhao, G., Souers, A.J., Voorbach, M., et alValidation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor. J. Med. Chem. 51(3), 380-383 (2008).

    Product Citations

    von Krusenstiern, A.N., Robson, R.N., Qian, N., et alIdentification of essential sites of lipid peroxidation in ferroptosis. Nat. Chem. Biol. 19(6), 719-730 (2023).

    Patel, R., Santoro, A., Hofer, P., et alATGL is a biosynthetic enzyme for fatty acid esters of hydroxy fatty acids. Nature (2021).