Acumapimod _p38 MAPK 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAcumapimodCat. No.: HY-16715CAS No.: 836683-15-9分式: CHNO分量: 385.42作靶点: p38 MAPK作通路: MAPK/ERK Pathway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 : 50 mg/mL (129.73 mM)* means soluble, but

2、saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.5946 mL 12.9729 mL 25.9457 mL5 mM 0.5189 mL 2.5946 mL 5.1891 mL10 mM 0.2595 mL 1.2973 mL 2.5946 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液

3、可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.49 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.49 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small Molec

4、ules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (6.49 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Acumapimod (BCT197)服活性的p38 MAP激酶抑制剂，对p38的IC50值于1 M。IC50 & Target IC50: less than 1 M (p38) 1体外研究 Acumapimod is an inhibitor of p38 with an IC50 value of less than 1 M.体内研究 BCT197 is an oral low-molecular-we

5、ight p38 inhibitor currently in development for the treatment of severalinflammatory conditions, including chronic obstructive pulmonary disease (COPD). Intermittent short-termdosing of BCT197 (75 mg on days 1 and 6) shows a marked improvement in lung function in COPD patients2.REFERENCES1. Norman P

6、, et al. Investigational p38 inhibitors for the treatment of chronic obstructive pulmonary disease. Expert Opin Investig Drugs.2015 Mar;24(3):383-92.2. De Buck S, et al. Population PK-PD Model for Tolerance Evaluation to the p38 MAP Kinase Inhibitor BCT197. CPT PharmacometricsSyst Pharmacol. 2015 Dec;4(12):691-700.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 4