JTT-654,916828-66-5

JTT-654 产品活性：JTT-654 是一种口服有效的选择性11β-羟基类固醇脱氢酶 1 型 (11β-HSD1) 抑制剂。在人、大鼠和小鼠重组酶中，JTT-654 对 11β-HSD1 的 IC50 分别为 4.65、0.97 和 0.74 nM。 JTT-654 对人重组酶表现出竞争性抑制。JTT-654 对人 11β-HSD2 的 IC50 值 > 30 μM（人 11β-HSD2 负责针对人 11β-HSD1 的逆反应）。JTT-654 通过抑制脂肪组织和肝脏 11β-HSD1 改善胰岛素抵抗和非肥胖 2 型糖尿病。 产品来源： www.medchemexpress.cn/jtt-654.html 研究领域：Metabolic Enzyme/Protease 作用靶点：11β-HSD In Vitro: JTT-654 (0.1-10 μM, 24 h) shows inhibitory effects on angiotensinogen production in Cortisone (HY-17461)-treated 3T3-L1 adipocytes. In Vivo: JTT-654 (1-10 mg/kg, Orally, single) shows inhibitory effect on liver and adipose tissue 11β-HSD1 activity. JTT-654 (1-10 mg/kg, Orally, once daily for 4 d) significantly attenuates the effect of Cortisone (HY-17461) in Rats. JTT-654 (1.5-15 mg/kg, Orally, twice daily, for 19 d) ameliorates insulin resistance and hyperglycemia in a non-obese type 2 diabetes rat model. 相关产品：Emodin | Carbenoxolone disodium | AZD 4017 | BVT 2733 | 11-Beta-hydroxyandrostenedione-d7 | ABT-384 | INCB13739 | BMS-770767 | AZD8329 | 18β-Glycyrrhetyl-3-O-sulfate | BMS-816336 | BVT-14225 | Necroptosis-IN-3 | 11β-HSD1-IN-1 | 11β-HSD1-IN-8 | HSD-016 | 11-Beta-hydroxyandrostenedione-d4 | 11β-HSD1-IN-10 | 11β-HSD1-IN-11 | 11β-HSD1-IN-12 | 11β-HSD1-IN-6 | 11β-HSD1-IN-7 | 11β-HSD1-IN-9 | 11β-HSD2-IN-1 | 11β-HSD2-IN-2 | AMG-221 | BI 187004