CM-4620 - CRAC Channel 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECM-4620Cat. No.: HY-101942CAS No.: 1713240-67-5分式: CHClFNO分量: 421.76作靶点: CRAC Channel作通路: Membrane Transporter/Ion Channel储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (237.10 m

2、M)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.93 mM); Suspended solution; Need ultrasonic and warming2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.93 mM); Suspended solution; Need ultrasonic and warming1/2 Master of Small Molecules 您边的抑制剂师www.MedChem

3、E3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.93 mM); Clear solution4. 请依序添加每种溶剂： 70%PEG300 30%(20% SBE-CD in saline)Solubility: 10 mg/mL (23.71 mM); Suspended solution; Need ultrasonicBIOLOGICAL ACTIVITY物活性 CM-4620钙离释放激活通道 (CRAC channel) 的抑制剂，其对 Orai1/STIM1 和 Orai2/STIM1 的 IC50 值分别为

4、 119 nM, 895 nM。IC50 & Target IC50: 119 nM (Orai 1/STIM1), 895 nM (Orai 1/STIM1) 1.体外研究 It is determined that CM-4620 (compound 1) inhibits Orai 1/STIM1 channels with an IC50 of 119 nM, andOrai2/STIM1 channels with an IC50 of 895 nM. It is more potent on Orai1 than Orai2-type CRAC channels. Inhuman

5、PBMCs, CM-4620 potently inhibits release of multiple cytokines which play important roles in T cells(IC50s, IFN : 138 nM, IL-4: 879 nM, IL-6: 135 nM, IL-1: 240 nM, IL-10: 303 nM, TNF: 225 nM, IL-2: 59nM, IL-17 120 nM) 1.体内研究 Mouse PACs are treated with CRAC inhibitors CM-4620 or GSK-7975A and monito

6、red for their rate ofCalcium uptake. Both CRAC inhibitors reduce the rate of store-operated Calcium entry into the ER to 50% ofcontrollevels upon treatment with 700 nM of inhibitor. CM-4620 blocks 100% of reuptake at 10 mM 1.REFERENCES1. ARYL SULFONOHYDRAZIDES. WO2016/138472Al.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400