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A-922500

Item № 10012708
CAS № 959122-11-3
Purity ≥95%
product image
                (CAS 959122-11-3)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $30.00 0.00
     5 mg $135.00 0.00
     10 mg $240.00 0.00
     25 mg $525.00 0.00

Pricing updated 2019-07-23. Prices are subject to change without notice.

Description
Synonyms
  • (1R,2R)-2-(4'-(3-phenylureido)biphenylcarbonyl)-cyclopentanecarboxylic acid

Diacylglycerol acyltransferases (DGATs) catalyze the final step in triglyceride synthesis. DGAT-1 deficient mice demonstrate a phenotype that is protective against the development of diet-induced obesity (DIO) or insulin resistance, implicating the actions of this enzyme in the development of such metabolic disorders. 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

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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
428.5
Purity
≥95%
Formulation
A crystalline solid
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

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 1 year
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Additional Information

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References & Product Citations
Product Description References

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

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