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Deucravacitinib
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。
Deucravacitinib图片
CAS NO:1609392-27-9
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
BMS-986165
产品介绍
BMS-986165 是一种高选择性、口服生物可利用的变构 TYK2 抑制剂,用于治疗自身免疫性疾病。它通过稳定调节 JH2 结构域来阻断受体介导的 Tyk2 激活,可抑制IL-12/23和 I 型IFN途径。它选择性结合 TYK2 假激酶 (JH2) 结构域,IC50为1.0 nM。

产品描述

BMS-986165 inhibits IL-12/23 and type I IFN pathways[1][2]. BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases. Which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain.

体外活性

BMS-986165 maintains excellent potency in human and mouse whole blood (IC50s=13 and 100 nM, respectively). Which shows no significant hERG inhibition in the flux assay (IC50>80 μM).BMS-986165 is differentiated from previous JAK inhibitors due its unique ability to selectively bind to the pseudokinase (JH2) domain of TYK2 and inhibit its function through an allosteric mechanism[1].

体内活性

BMS-986165 as a high affinity JH2 ligand and potent allosteric inhibitor of TYK2. In addition to unprecedented JAK isoform and kinome selectivity, BMS-986165 shows excellent pharmacokinetic properties with minimal profiling liabilities and is efficacious in several murine models of autoimmune disease. On the basis of these findings, BMS-986165 appears differentiated from all other reported JAK inhibitors and has been advanced as the first pseudokinase-directed therapeutic in clinical development as an oral treatment for autoimmune diseases[1].

Cas No.

1609392-27-9

分子式

C20H22N8O3

分子量

425.46

别名

BMS-986165

储存和溶解度

DMSO:32.5mg/ml (76.39 Mm),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years