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首页-小分子抑制剂&激动剂-GPCR-Cannabinoid Receptor-JD-5037
JD-5037

Chemical Structure : JD-5037

CAS No.: 1392116-14-1

JD-5037 (JD 5037;JD5037)

货号: PC-45531Not For Human Use, Lab Use Only.

JD-5037 is a potent, selective and peripherally restricted cannabinoid-1 (CB1) receptor blocker with IC50 of 2 nM, does not inhibit CB2 receptor (IC50>1000 nM).

规格 价格 库存 数量
5 mg ¥780 In stock
10 mg ¥1180 In stock
25 mg ¥1980 In stock
50 mg ¥2980 In stock
100 mg Get quote

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

JD-5037 is a potent, selective and peripherally restricted cannabinoid-1 (CB1) receptor blocker with IC50 of 2 nM, does not inhibit CB2 receptor (IC50>1000 nM).
JD-5037 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-5037 showed little brain presence as indicated by tissue distribution and receptor occupancy studies.
JD-5037 (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 572.506
分子式 C27H27Cl2N5O3S
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

DMSO: 10 mM

Chemical Name/SMILES

Butanamide, 2-[[[(4S)-3-(4-chlorophenyl)-4,5-dihydro-4-phenyl-1H-pyrazol-1-yl][[(4-chlorophenyl)sulfonyl]amino]methylene]amino]-3-methyl-, (2S)-

参考文献

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

2. Tam J, et al. Cell Metab. 2012 Aug 8;16(2):167-79.

3. Knani I, et al. Mol Metab. 2016 Oct 22;5(12):1187-1199.

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