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RTICBM-189
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
RTICBM-189图片
CAS NO:551909-15-0
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
RTICBM-189 是一种有效的，可透过血脑屏障的大麻素 1 型 (CB1) 受体变构调节剂，在 Ca2+ 动员试验中 pIC50 为 7.54。RTICBM-189 对 hCB1 和 mCB1 的 pIC50 分别为 5.29 和 6.25。RTICBM-189 显著且选择性地减弱大鼠可卡因寻求行为的恢复。
Cas No.551909-15-0
分子式C15H14Cl2N2O
分子量309.19
溶解度DMSO : 100 mg/mL (323.43 mM; Need ultrasonic)
储存条件4°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the cocaine-seeking behavior in rats[1].

RTICBM-189 (10 mg/kg; i.p.) significantly and selectively attenuates reinstatement of the cocaine-seeking behavior in rats[1].RTICBM-189 (10 mg/kg; i.p.) rapidly absorbs into systemic circulation, with peak plasma concentration (Cmax,plasma=288.4 ng/mL) observed at tmax,plasma of 0.4 h post-dose. Peak brain levels are also reached at tmax,brain of 0.4 h with a significantly higher Cmax,brain value of 594.6 ng/mL in the brain[1].

[1]. Nguyen T, et al. Development of 3-(4-Chlorophenyl)-1-(phenethyl)urea Analogues as Allosteric Modulators of the Cannabinoid Type-1 Receptor: RTICBM-189 is Brain Penetrant and Attenuates Reinstatement of Cocaine-Seeking Behavior [published online ahead of print, 2021 Dec 20]. J Med Chem. 2021;10.1021/acs.jmedchem.1c01432.