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AZD7687

CAS：1166827-44-6

产品活性：AZD7687 is a potent and selective DGAT1 inhibitor with an IC50 value of 80 nM (hDGAT1). IC50 value: 80 nM [1] Target: DGAT1 in vitro: Plasma AZD7687 exposure was measured repeatedly. AZD7687 markedly reduced postprandial TAG excursion with a steep concentration-effect relationship [2]. Postprandial serum TAG excursion was measured during 8 h after a standardized mixed meal with fat energy content of 60% (SMM 60%; five cohorts, 1-20 mg), before (baseline) and after dosing, to assess effects on gut DGAT1 activity. in vivo: Multiple doses of AZD7687 (1, 2.5, 5, 10 and 20 mg/day, n=6 or n=12 for each) or placebo (n=20) were administered for 1 week. With AZD7687 doses >5 mg/day, gastrointestinal (GI) side effects increased; 11/18 of these participants discontinued treatment owing to diarrhoea[3]. Dose-dependent reductions in postprandial serum TAG were demonstrated with AZD7687 doses ≥5mg compared with placebo (p<0.01). Significant (p<0.001) increases in plasma GLP-1 and PYY levels were seen at these doses, but no clear effect on gastric emptying was demonstrated at the end of treatment.

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品牌介绍：
☆ TargetMol品牌专业提供各领域信号通路小分子抑制剂、拮抗剂、天然产物、药物筛选化合物。
☆ 产品适应在癌症、免疫学、心血管系统、呼吸、神经科学等多项科学领域的研发使用，超过660万种小分子化合物。
☆ 提供20000多个小分子抑制剂、天然产物和200多个化合物库。
☆ 配备完善的化学合成和生物实验室，可分别提供高品质小分子抑制剂和药物筛选技术服务。
☆ 每批产品都有严格的NMR和HPLC技术检测，以保证产品高纯度高质量。

原创作者：上海陶术生物科技有限公司