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CAS No.: 836683-15-9

Acumapimod Catalog No. CSN19014

Synonyms: BCT197;BCT197A2201

Acumapimod is an orally active p38 MAP kinase inhibitor, with an IC50 of less than 1 μM for p38α.

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生物活性

实验方案

技术信息

生物活性

描述p38 mitogen-activated protein kinases (p38 MAPK, p38) consist of 4 subunits: p38α, p38β, p38γ and p38δ. They play a well-recognized role in regulating intracellular signaling transduction in mammalian cells. p38 MAPK induces a variety of intracellular responses associated with neuropathic pain and other chronic pain^[2]. Acumapimod（BCT197） is an orally active inhibitor of p38α MAPK (IC50 <1 μM). When examining BCT197 in vivo, and comparing to vehicle-treated animals, reduced weight loss, improvement in survival and lack of impaired viral control was observed at BCT197 concentrations relevant to those being used in clinical trials of acute exacerbations of chronic obstructive pulmonary disease; at higher concentrations of BCT197 these effects were reduced. BCT197 improved survival and weight loss compared to vehicle, but to a lesser degree than either oseltamivir or dexamethasone. It was also demonstrated that both dexamethasone and the higher dose of BCT197 increased viral load 7 days p.i. The lower dose of BCT197, which is more clinically relevant, remained comparable to vehicle treatment^[3]. BCT197 was found to be a low clearance drug (1.76 L/h),with linearity in oral drug clearance (CL/F) demonstrated over the entire dose range tested (0.1–75 mg). No relevant differences in relative bioavailability between these formulations were seen. BCT197 exhibited an apparent absorption plateau, with a tendency to less than dose-proportional increase in peak drug concentration (Cmax)^[4].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03498170	Interaction	Phase 1	Completed	-	United States, Florida ... more >> inVentiv Health Clinical Research Services LLC Miami, Florida, United States, 33136 Collapse <<
NCT02926326	Interaction	Phase 1	Completed	-	United Kingdom ... more >> BioKinetic Europe Ltd Belfast, United Kingdom, BT2 7BA Collapse <<

参考文献

[1] Norman P. Selective JAK inhibitors in development for rheumatoid arthritis. Expert Opin Investig Drugs. 2014 Aug;23(8):1067-77.
[2] X Lin,et al. p38 MAPK: a potential target of chronic pain. Curr Med Chem. 2014;21(38):4405-18.
[3] Growcott E J , Bamba D , Galarneau J . R , et al. The effect of P38 MAP kinase inhibition in a mouse model of influenza[J]. Journal of Medical Microbiology, 2018, 67(3) .
[4] De Buck S , Hueber W , Vitaliti A , et al. Population PK-PD Model for Tolerance Evaluation to the p38 MAP Kinase Inhibitor BCT197[J]. CPT: Pharmacometrics & Systems Pharmacology, 2015, 4(12):691-700.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5946 mL
- 12.9729 mL
- 25.9458 mL
- 5 mM
- 0.5189 mL
- 2.5946 mL
- 5.1892 mL
- 10 mM
- 0.2595 mL
- 1.2973 mL
- 2.5946 mL

技术信息

CAS号

836683-15-9

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H19N5O2

运输

蓝冰

分子量

385.42

别名

BCT197;BCT197A2201

溶解度

DMSO	48.0 mg/mL (124.5 mM)

动物实验配方

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