CAS:1415823-73-2Evobrutinib

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Evobrutinib Cat No. FB11211Cas No. 1415823-73-2

Synonyms: M2951;MSC 2364447C

Evobrutinib is a highly selective inhibitor of the Bruton's tyrosine kinase (BTK), which is important in the development and functioning of various immune cells including B lymphocytes and macrophages. Preclinical research suggests it may be therapeutically useful in certain autoimmune diseases.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3282 mL
- 11.6411 mL
- 23.2821 mL
- 5 mM
- 0.4656 mL
- 2.3282 mL
- 4.6564 mL
- 10 mM
- 0.2328 mL
- 1.1641 mL
- 2.3282 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号

1415823-73-2

储存条件

粉末: -20°C 3 年

液体: -80°C 12 月

分子式

C25H27N5O2

运输

蓝冰

分子量

429.51

别名

M2951;MSC 2364447C

溶解度

DMSO	86.0 mg/mL (200.2 mM)
Water	Insoluble
Ethanol	10.0 mg/mL (23.3 mM)

动物实验配方

靶点数据

生物活性

描述Bruton's tyrosine kinase (BTK), a member of the Tec family of tyrosine kinases and expressed in B cells, macrophages, and monocytes but not in T cells, plays a crucial role in signaling through the B cell receptor (BCR) and the Fcγ receptor (FcγR) in B cells and myeloid cells, respectively. Evobrutinib, used for the treatment of autoimmune diseases, is a potent and irreversibly covalent BTK inhibitor with an IC₅₀ of 8.9 nM. In a B cell stimulation assay in normal C57BL/6 mice, evobrutinib (1 mg/kg orally) achieved a B cell inhibition of 71% and 25% at 1 and 24 h. Evaluation of evobrutinib PK in mice, rats, and dogs indicated that evobrutinib is rapidly absorbed after oral administration, with C_max reached between 0.25 and 1 h. In a rat collagen-induced arthritis (CIA) model, disease-induced ankle-swelling was significantly reduced (P≤0.05) for rats treated with evobrutinib 3 mg/kg (days 11−17), 10 mg/kg (days 11−17), 30 mg/kg (days 10−17), or methotrexate (days 11−17), compared with vehicle. Ankle histopathology scores were also reduced with evobrutinib in a dose-dependent manner compared to vehicle and the IC₅₀ for evobrutinib was 5.180 mg/kg.
作用机制Evobrutinib covalently binds to Cys481 of the BTK kinase domain.