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Tolebrutinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tolebrutinib图片
CAS NO:1971920-73-6
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
50 mg电议
100 mg电议
200 mg电议

产品名称
PRN2246
SAR442168
产品介绍
Tolebrutinib 是一种选择性、有效的、具有口服活性、可透过血脑屏障的布鲁顿氏酪氨酸激酶抑制剂,能够作用于 Ramos B 细胞 (IC50:0.4 nM)、HMC 小胶质细胞 (IC50:0.7 nM)。它对中枢神经系统免疫具有功效。它可用于多发性硬化症的研究。

产品描述

Tolebrutinib is a potent, selective, orally active and brain-penetrant Bruton tyrosine kinase (BTK) inhibitor(IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively). It exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS).

体外活性

PRN2246 inhibits microglial FcγR activation through durable occupancy of BTK, with an IC50 of 157 nM.?PRN2246 blocks the BCR-mediated activation (IC50=10 nM) and Fc receptor activation (IC50=166 and 9.6 nM for FcεR and FcγR, repectively) of immune cells[1].

体内活性

PRN2246 produces dose-dependent protection from in myelin oligodendrocyte glycoprotein (MOG)-induced experimental autoimmune encephalomyelitis (EAE) model[1]

Cas No.

1971920-73-6

分子式

C26H25N5O3

分子量

455.518

别名

PRN2246;SAR442168

储存和溶解度

DMSO:100 mg/mL (219.53 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years