Acumapimod _p38 MAPK 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAcumapimodCat. No.: HY-16715CAS No.: 836683-15-9分式: CHNO分量: 385.42作靶點(diǎn): p38 MAPK作通路: MAPK/ERK Pathway儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (129.73 mM)* means soluble, but

2、saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液

3、可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.49 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.49 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Molec

4、ules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (6.49 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Acumapimod (BCT197)服活性的p38 MAP激酶抑制劑，對(duì)p38的IC50值于1 M。IC50 & Target IC50: less than 1 M (p38) 1體外研究 Acumapimod is an inhibitor of p38 with an IC50 value of less than 1 M.體內(nèi)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