CMPD101 hydrochloride

产品名称：

1941168-71-3
CMPD101 hydrochloride
3-((4-Methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)methylamino)-N-(2-(trifluoromethyl)benzyl)benzamide
Takeda101 hydrochloride
Cpd101 hydrochloride
Compound 101 hydrochloride
3-[[[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide hydrochloride

产品介绍：

产品说明

生化/生理作用

CMPD101 is an active site-targeting, potent and subtype-selective G protein-coupled receptor kinase GRK2 & GRK3 inhibitor (human GRK2/3 IC₅₀ = 54/32 nM with 3 μM ATP and tubulin dimer as substrate; bovine GRK2 IC₅₀ = 290 nM with 0.5 mM ATP and bROS as substrate; no GRK1/5 inhibition at 125 μM). CMPD101 selectively inhibits GPR39 agonist-induced β-arrestin recruitment (by 94% at 10 μM against 30 μM GPR39-C3/50 μM ZnCl2), but not cAMP pathway desensitization in cultures and prevents β-arrestin2-biased D2R ligand UNC9994(1 μg/side bilateral local injection) from blocking NMDAR antagonist PCP (6 mg/kg i.p.)-induced locomotion (60%/12% blockage without/with 0.5 μg CMPD101 co-injection) in mice in vivo.

基本信息

经验(实验)分子式	C₂₄H₂₁N₆OF₃ · HCl
分子量	502.92

产品性质

质量水平	100
测定	≥98% (HPLC)
形式	powder
储存条件	desiccated
颜色	white to beige
溶解性	DMSO: 2 mg/mL, clear
储存温度	2-8℃
SMILES string	CN1C(CNC2=CC=CC(C(NCC3=CC=CC=C3C(F)(F)F)=O)=C2)=NN=C1C4=CC=NC=C4.Cl

安全信息

储存分类代码	11 - Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable