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SHR0302 (ARQ252) 是一种具有口服活性的 JAK 抑制剂。它对 JAK1的结合力是 JAK2的 10 倍以上,是 JAK3的 77 倍,是 Tyk2的 420 倍。它抑制JAK1-STAT3磷酸化并诱导肝星状细胞凋亡,具有抗增殖和抗炎作用。
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SHR0302 (ARQ252) 是一种具有口服活性的 JAK 抑制剂。它对 JAK1的结合力是 JAK2的 10 倍以上,是 JAK3的 77 倍,是 Tyk2的 420 倍。它抑制JAK1-STAT3磷酸化并诱导肝星状细胞凋亡,具有抗增殖和抗炎作用。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 1,650 | 现货 | |
5 mg | ¥ 4,130 | 现货 | |
10 mg | ¥ 5,880 | 现货 | |
25 mg | ¥ 8,750 | 现货 | |
50 mg | ¥ 11,800 | 现货 | |
100 mg | ¥ 15,900 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 4,590 | 现货 |
产品描述 | SHR0302 (ARQ252) is a JAK inhibitor that binds JAK1 with stronger affinity than others (Selectivity for JAK1 is more than 10 times for JAK2, 77 times for JAK3, 420 times for Tyk2). |
体外活性 | SHR0302 (1nM-10μM) exerted an inhibitory effect on the activation, proliferation and migration of hepatic stellate cells (HSCs). SHR0302 induced the apoptosis of HSCs. The pharmacological inhibition of the JAK1/signal transducer and activator of transcription (STAT)3 pathway led to the disruption of functions essential for HSC[1]. |
体内活性 | SHR0302 may attenuate the severity of AA rats, partially through reducing Th17 function and total B cell proportion by inhibiting JAK1-STAT3 phosphorylation[2]. |
别名 | ARQ252 |
分子量 | 414.48 |
分子式 | C18H22N8O2S |
CAS No. | 1445987-21-2 |
Smiles | [H][C@@]12C[C@H](C[C@]1([H])CN(C2)C(=O)Nc1nc(OC)ns1)N(C)c1ncnc2[nH]ccc12 |
密度 | 1.507 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 30 mg/mL (72.38 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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