959122-11-3
A 922500
CAS: 959122-11-3
Molecular Formula: C26H24N2O4
959122-11-3 - Names and Identifiers
| Name | A 922500 |
| Synonyms | A922500 A 922500 DGAT-1 inhibitor DGAT-1 Inhibitor 4a A922500(DGAT-1 Inhibitor 4a) Diacyl glycerolacyltransferase 1 inhibitor enylureido)biphenyl(1R,2R)-2-(4'-(3-phcarbonyl)cyclopentanecarboxylic acid (1R,2R)-2-(4'-(3-phenylureido)biphenylcarbonyl)cyclopentanecarboxylic acid (1R,2R)-2-[[4'-[[(Phenylamino)carbonyl]amino][1,1'-biphenyl]-4-yl]carbonyl]cyclopentanecarboxylic acid |
| CAS | 959122-11-3 |
959122-11-3 - Physico-chemical Properties
| Molecular Formula | C26H24N2O4 |
| Molar Mass | 428.48 |
| Density | 1.323 |
| Solubility | Soluble in DMSO |
| Appearance | Light yellow solid |
| Storage Condition | -20°C |
| Use | 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. Acyl CoA/diacylglycerol acyltransferase (DGAT) 1 is one of two known DGAT enzymes that catalyze the final and only committed step in triglyceride biosynthesis. |
| Target | DGAT2; human DGAT-1; mouse DGAT-1; |
| In vitro study | A922500 inhibits relative family members acetyl-coenzyme A cholesterol acetyltransferase -1 and -2 with an IC50 of 296 μm. A922500 effectively inhibits huDGAT-1 and mseDGAT-1. |
| In vivo study | A922500 (0.03,0.3, and 3 mg/kg) was administered orally for 14 days to Zucker obese rats and diet-induced dyslipidemic hamsters. A922500 at a dose of 3 mg/kg significantly reduced serum triglycerides in Zucker obese rats (39%) and hyperlipidemic hamsters (53%). These changes in serum triglycerides were accompanied by a significant decrease in free fatty acid levels, which were reduced by 32% and 55% in Zucker obese rats and hyperlipidemic hamsters, respectively. In addition, A 922500(3 mg/kg) significantly increased HDL-cholesterol (25%) in Zucker obese rats. Long-term administration of A 922500 to DIO mice results in weight loss and hepatic triglyceride reduction, and dose-dependent depletion of serum triglyceride under lipid stimulation, thereby reproducing DGAT-1(-/-) the main phenotypic characteristics of mice. A 922500 (0.03, 0.3 and 3 mg/kg, p.o.) dose-dependently attenuated the rise in maximal postprandial serum triglyceride concentrations. |
959122-11-3 - Risk and Safety
| Risk Codes | R25 - Toxic if swallowed R36 - Irritating to the eyes R50 - Very Toxic to aquatic organisms |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S61 - Avoid release to the environment. Refer to special instructions / safety data sheets. |
| UN IDs | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
959122-11-3 - Reference
| Reference Show more | 1: Tsuda N, Kumadaki S, Higashi C, Ozawa M, Shinozaki M, Kato Y, Hoshida K,Kikuchi S, Nakano Y, Ogawa Y, Furusako S. Intestine-targeted DGAT1 inhibitionimproves obesity and insulin resistance without skin aberrations in mice. PLoSOne. 2014 Nov 18;9(11):e112027. doi: 10.1371/journal.pone.0112027. eCollection2014. PubMed PMID: 25405858; PubMed Central PMCID: PMC4236014. 2: King AJ, Segreti JA, Larson KJ, Souers AJ, Kym PR, Reilly RM, Collins CA,Voorbach MJ, Zhao G, Mittelstadt SW, Cox BF. In vivo efficacy of acyl CoA:diacylglycerol acyltransferase (DGAT) 1 inhibition in rodent models ofpostprandial hyperlipidemia. Eur J Pharmacol. 2010 Jul 10;637(1-3):155-61. doi:10.1016/j.ejphar.2010.03.056. Epub 2010 Apr 10. PubMed PMID: 20385122. 3: King AJ, Segreti JA, Larson KJ, Souers AJ, Kym PR, Reilly RM, Zhao G,Mittelstadt SW, Cox BF. Diacylglycerol acyltransferase 1 inhibition lowers serumtriglycerides in the Zucker fatty rat and the hyperlipidemic hamster. J Pharmacol Exp Ther. 2009 Aug;330(2):526-31. doi: 10.1124/jpet.109.154047. Epub 2009 May 28.PubMed PMID: 19478132. |
959122-11-3 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.334 ml | 11.669 ml | 23.338 ml |
| 5 mM | 0.467 ml | 2.334 ml | 4.668 ml |
| 10 mM | 0.233 ml | 1.167 ml | 2.334 ml |
| 5 mM | 0.047 ml | 0.233 ml | 0.467 ml |
Last Update：2024-01-02 23:10:35
959122-11-3 - Reference Information
| biological activity | A922500 (DGAT-1 Inhibitor 4a) is a DGAT-1 Inhibitor in humans and mice, the IC50 was 7 nM and 24 nM, respectively, which was higher than that of the related acyl transferase, hERG and anti target panel. |
| Target | Value |
| human DGAT-1 () | 7 nM |
| mouse DGAT-1 () | 24 nM |
Last Update：2024-04-09 21:54:55
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Product Name: A 922500 Request for quotation
CAS: 959122-11-3
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
CAS: 959122-11-3
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: DGAT-1 inhibitor Visit Supplier Webpage Request for quotationCAS: 959122-11-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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