S29693 |
JD-5037 |
源叶(MedMol) | 98% |
- 产品描述: JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM
- 靶点: Cannabinoid Receptor;CannabinoidReceptor
- 体内研究:
JD5037 (3 mg/kg/d, i.p.) induces equal reductions in body weight, attenuates the HFD-induced hyperglycemia, and reduces the HFD-induced hepatic injury and steatosis in obese Magel2-null mice. JD5037 (3 mg/kg/day, p.o.) significantly reduces the size of tumors and abrogates the tumor in DEN-treated mice. JD5037 attenuates the AEA levels in HCC samples from mice.
- 动物实验: Mice: JD-5037 is formulated in vehicle (V; 1% Tween80, 4% DMSO, 95% Saline). Obese mice are treated chronically (28 d) with vehicle (V; 1% Tween80, 4% DMSO, 95% Saline), JD5037, or SLV319 at a dose of 3 mg/kg, i.p. Body weight and food intake are monitored daily. Mice are euthanized by cervical dislocation under anesthesia; the brain, hypothalamus, liver, and combined fat pads are removed, weighed, and snap-frozen, and trunk blood is collected for determining the endocrine and biochemical parameters
- 参考文献:
1. Chorvat RJ.etal.Peripherally restricted CB1 receptor blockers.Bioorg Med Chem Lett. 2013 Sep 1;23(17):4751-60. 2. Knani I,etal.Targeting the endocannabinoid/CB1 receptor system for treating obesity in Prader-Willi syndrome.Mol Metab. 2016 Oct 22;5(12):1187-1199. 3. Mukhopadhyay B,etal.Cannabinoid receptor 1 promotes hepatocellular carcinoma initiation and progression through multiple mechanisms.Hepatology. 2015 May;61(5):1615-26. 4.Tan S, Liu H, Ke B, et al. The peripheral CB1 receptor antagonist JD5037 attenuates liver fibrosis via a CB1 receptor/β‐arrestin1/Akt pathway[J]. British Journal of Pharmacology. 2020, 177(12): 2830-2847.
- 溶解性: Soluble in DMSO
- 保存条件: 2-8℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 1.747 ml 8.733 ml 17.467 ml 5 mM 0.349 ml 1.747 ml 3.493 ml 10 mM 0.175 ml 0.873 ml 1.747 ml 50 mM 0.035 ml 0.175 ml 0.349 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)