Molecular Formula | C27H27Cl2N5O3S |
Molar Mass | 572.51 |
Density | 1.40±0.1 g/cm3(Predicted) |
Boling Point | 721.6±70.0 °C(Predicted) |
Solubility | DMSO |
pKa | 10.63±0.60(Predicted) |
Storage Condition | 2-8℃ |
MDL | MFCD30533451 |
Use | JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM. |
Target | CB1 |
In vivo study | 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. |
Reference Show more | 1. Chorvat RJ. Peripherally restricted CB1 receptor blockers. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4751-60.2. Knani I, et al. 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, et al. Cannabinoid receptor 1 promotes hepatocellular carcinoma initiation and progression through multiple mechanisms. Hepatology. 2015 May;61(5):1615-26. |
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 |
5 mM | 0.035 ml | 0.175 ml | 0.349 ml |
biological activity | JD-5037 is a cannabinoid-1 receptor blocker, the IC50 value for CB1 receptor is 2 nM, and the IC50 value for CB2 receptor is greater than 1000 nM. |
target | TargetValue CB1 receptor () 2 nM |
Target | Value |
CB1 receptor () | 2 nM |
in vivo study | 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. |