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别名 ARQ252
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) | ¥ 3,780 | 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/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 30 mg/mL (72.38 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (4.83 mM), Sonication is recommeded. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
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以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
对于不同动物的给药剂量换算,您也可以参考 更多