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首页-小分子抑制剂&激动剂-GPCR-Cannabinoid Receptor-JD-5006
JD-5006

Chemical Structure : JD-5006

CAS No.: 1148142-42-0

JD-5006 (JD5006)

货号: PC-20518Not For Human Use, Lab Use Only.

JD-5006 is a potent, selective and peripherally restricted cannabinoid-1 (CB1) receptor blocker with IC50 of 18 nM, does not inhibit CB2 receptor (IC50>5000 nM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

JD-5006 is a potent, selective and peripherally restricted cannabinoid-1 (CB1) receptor blocker with IC50 of 18 nM, does not inhibit CB2 receptor (IC50>5000 nM).
JD-5006 was also characterized as an inverse agonist in forskolin-stimulated CHO cells over- expressing CB1-receptors by its ability to affect cAMP with EC50 of 46 nM.
JD-5006 showed little brain presence as indicated by tissue distribution and receptor occupancy studies.
JD-5006 (20 mg/kg PO) normalized triglyceride levels, liver mass and ALT as well a beneficial effect on glycemic control in model of diabetes.

物理化学性质&存储条件

分子量 530.42
分子式 C24H21Cl2N5O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

O=C(N)CN/C(N1N=C(C2=CC=C(Cl)C=C2)C(C3=CC=CC=C3)C1)=N\S(=O)(C4=CC=C(Cl)C=C4)=O

参考文献

1. Robert J Chorvat, et al. Bioorg Med Chem Lett. 2012 Oct 1;22(19):6173-80.

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