AZD7687 - CAS 1166827-44-6
Catalog number: 1166827-44-6
Category: Inhibitor
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AZD7687 is a potent and selective DGAT1 inhibitor with an IC50 value of 80 nM (hDGAT1).
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1.Proof of mechanism for the DGAT1 inhibitor AZD7687: results from a first-time-in-human single-dose study.
Denison H1, Nilsson C, Kujacic M, Löfgren L, Karlsson C, Knutsson M, Eriksson JW. Diabetes Obes Metab. 2013 Feb;15(2):136-43. doi: 10.1111/dom.12002. Epub 2012 Sep 30.
AIMS: Inhibition of diacylglycerol acyltransferase 1 (DGAT1), which catalyses the final step in triacylglycerol (TAG) assembly, is suggested as a treatment for type 2 diabetes and obesity based on animal data indicating insulin sensitization and weight reduction. This first-time-in-human single ascending dose study explored the safety, tolerability, pharmacokinetics and pharmacodynamics of the selective DGAT1 inhibitor AZD7687.
2.Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
Barlind JG1, Bauer UA, Birch AM, Birtles S, Buckett LK, Butlin RJ, Davies RD, Eriksson JW, Hammond CD, Hovland R, Johannesson P, Johansson MJ, Kemmitt PD, Lindmark BT, Morentin Gutierrez P, Noeske TA, Nordin A, O'Donnell CJ, Petersson AU, Redzic A, Turnbu J Med Chem. 2012 Dec 13;55(23):10610-29. doi: 10.1021/jm301296t. Epub 2012 Nov 21.
A new series of pyrazinecarboxamide DGAT1 inhibitors was designed to address the need for a candidate drug with good potency, selectivity, and physical and DMPK properties combined with a low predicted dose in man. Rational design and optimization of this series led to the discovery of compound 30 (AZD7687), which met the project objectives for potency, selectivity, in particular over ACAT1, solubility, and preclinical PK profiles. This compound showed the anticipated excellent pharmacokinetic properties in human volunteers.
3.Diacylglycerol acyltransferase 1 inhibition with AZD7687 alters lipid handling and hormone secretion in the gut with intolerable side effects: a randomized clinical trial.
Denison H1, Nilsson C, Löfgren L, Himmelmann A, Mårtensson G, Knutsson M, Al-Shurbaji A, Tornqvist H, Eriksson JW. Diabetes Obes Metab. 2014 Apr;16(4):334-43. doi: 10.1111/dom.12221. Epub 2013 Oct 31.
AIM: Inhibition of diacylglycerol acyltransferase 1 (DGAT1) is a potential treatment modality for patients with type 2 diabetes mellitus and obesity, based on preclinical data suggesting it is associated with insulin sensitization and weight loss. This randomized, placebo-controlled, phase 1 study in 62 overweight or obese men explored the effects and tolerability of AZD7687, a reversible and selective DGAT1 inhibitor.
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CAS 1166827-44-6 AZD7687

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