| 货号 | 12053-1mg |
| 描述 | JD5037 is an inverse agonist of peripheral cannabinoid 1 (CB1) receptors (Ki = 0.35 nM).1 It displays >700-fold selectivity for CB1 over CB2, >1,000-fold selectivity over a panel of 70 receptors, transporters, and ion channels, and low blood-brain barrier penetrance.2,1 JD5037 is orally bioavailable and reduces food intake, body weight, and hormonal/metabolic abnormalities in diet-induced obese mice.3,1 JD5037 reverses hyperphagia, reduces body weight, and improves metabolic parameters in Magel2-null mice, a model of Prader-Willi syndrome.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Tam, J.,Cinar, R.,Liu, J., et al. Peripheral cannabinoid-1 receptor inverse agonism reduces obesity by reversing leptin resistance. Cell Metabolism 16, 167-179 (2012). 2.Chorvat, R.J.,Berbaum, J.,Seriacki, K., et al. JD-5006 and JD-5037: Peripherally restricted (PR) cannabinoid-1 receptor blockers related to SLV-319 (Ibipinabant) as metabolic disorder therapeutics devoid of CNS liabilities. Bioorg. Med. Chem. Lett. 22(19), 6173-6180 (2012). 3.Cinar, R.,Godlewski, G.,Liu, J., et al. Hepatic cannabinoid-1 receptors mediate diet-induced insulin resistance by increasing de novo synthesis of long-chain ceramides. Hepatology 59(1), 143-153 (2014). 4.Knani, I.,Earley, B.J.,Udi, S., et al. Targeting the endocannabinoid/CB1 receptor system for treating obesity in Prader-Willi syndrome. Mol. Metab. 5(12), 1187-1199 (2016). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 572.5 |
| 分子式 | C27H27Cl2N5O3S |
| CAS号 | 1392116-14-1 |
| 稳定性 | ≥ 2 years |
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