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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-H018
H018

Chemical Structure : H018

CAS No.: 2549180-90-5

H018 (RAI-20)

货号: PC-26282Not For Human Use, Lab Use Only.

H018 (RAI-20) is a highly potent, selective JAK1/2 inhibitor with IC50 of 15.1/22.7 nM, >10-fold and 20-fold selective over JAK3 amd TYK2, displays robust anti-arthritic efficacy.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

H018 (RAI-20) is a highly potent, selective JAK1/2 inhibitor with IC50 of 15.1/22.7 nM, >10-fold and 20-fold selective over JAK3 amd TYK2, displays robust anti-arthritic efficacy.
H018 (RAI-20) shows inhibitory activity against Ba/F3 cells with IC50 of 1.21 uM, nearly 6 times more potent than Filgotinib.
H018 (RAI-20) inhibits the expression of pSTAT1 induced by IL-6 with IC50 of 1.45 uM in human whole blood.
H018 (RAI-20) (2, 3, 5, and 10 mg/kg) significantly reduced the hind paw volume in CIA model.

物理化学性质&存储条件

分子量 448.53
分子式 C20H21FN4O3S2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Cyclopropanecarboxamide, N-[5-[5-[(1,1-dioxido-4-thiomorpholinyl)methyl]-2-thienyl]imidazo[1,2-a]pyridin-2-yl]-2-fluoro-, (1R,2S)-rel-

参考文献

1. Haifeng Zhu, et al. Eur J Med Chem. 2026 Mar 2:309:118729.

2. Patent CN111892592 A 2020-11-06.

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