|[6-碘-2-甲基-1-[2-(4-吗啉基)乙基]-1H-吲哚-3-基](4-甲氧基苯基)甲酮|CsnPharm

CAS No.: 164178-33-0

(6-Iodo-2-methyl-1-(2-morpholinoethyl)-1H-indol-3-yl)(4-methoxyphenyl)methanone Catalog No. CSN12849

Synonyms: 6-Iodopravodoline;iodopravadoline

AM630 is a selectivity CB2 antagonist with Ki of 31.2 nM with a > 150 fold selectivity over CB1 receptor.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Cannabinoid Receptor 2

Ki:31.2nM Cannabinoid Receptor 1

Ki:4680nM
描述AM630 (iodopravadoline), a novel aminoalkylindole. AM630 behaved as a competitive antagonist of CP 55,940, WIN 55,212-2, anandamide and (R)-(+)-arachidonyl-1'-hydroxy-2'-propylamide (AM356), producing rightward shifts in the log concentration response curves of these cannabinoid receptor agonists. AM630 was markedly more potent as an antagonist of delta 9-THC and CP 55,940 (Kd = 14.0 and 17.3 nM respectively) than as an antagonist of WIN 55,212-2, AM356 or anandamide (Kd = 36.5, 85.9 and 278.8 nM respectively)^[3]. AM630 is a protean ligand that can target a constitutively active form of the hCB(2) receptor (R*) with low affinity to produce agonism or neutral antagonism and a constitutively inactive form of this receptor (R) with much higher affinity to produce inverse agonism, and that the constitutive activity of whole cells is decreased less by pre-incubation with AM630 than with the higher-efficacy inverse agonist, SR144528^[4]. AM251 and AM630 activated trigeminal (TG) sensory neurons in a concentration-dependent fashion (threshold 1 μM). AM630 (1-100 μM), but not AM251, was a significantly more potent agonist in cells co-expressing both TRPA1 and TRPV1 channels^[5].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9827 mL
- 9.9135 mL
- 19.8271 mL
- 5 mM
- 0.3965 mL
- 1.9827 mL
- 3.9654 mL
- 10 mM
- 0.1983 mL
- 0.9914 mL
- 1.9827 mL

技术信息

CAS号

164178-33-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H25IN2O3

运输

蓝冰

分子量

504.36

别名

6-Iodopravodoline;iodopravadoline

溶解度

DMSO	50.0 mg/mL (99.1 mM) warming

动物实验配方

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靶点	Description	IC50
Cannabinoid Receptor 2		Ki:31.2nM
Cannabinoid Receptor 1		Ki:4680nM

(6-Iodo-2-methyl-1-(2-morpholinoethyl)-1H-indol-3-yl)(4-methoxyphenyl)methanone Catalog No. CSN12849

靶点选择性

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