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ASK1-IN-2 是一种口服有活性的凋亡信号调节激酶 1 抑制剂(IC50:32.8 nM)。它可用于研究溃疡性结肠炎。
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ASK1-IN-2 是一种口服有活性的凋亡信号调节激酶 1 抑制剂(IC50:32.8 nM)。它可用于研究溃疡性结肠炎。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 669 | 现货 | |
5 mg | ¥ 1,650 | 现货 | |
10 mg | ¥ 2,650 | 现货 | |
25 mg | ¥ 4,770 | 现货 | |
50 mg | ¥ 7,160 | 现货 | |
100 mg | ¥ 9,660 | 现货 | |
500 mg | ¥ 19,300 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,820 | 现货 |
产品描述 | ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. ASK1-IN-2 can potentially be used as a therapeutic strategy for ulcerative colitis[1]. |
靶点活性 | ASK1:32.8 nM (IC50) |
体外活性 | ASK1-IN-2 displays potent anti-ASK1 kinase activity and strong inhibitory effect on ASK1 in AP1-HEK293 cells with inhibition rate of 95.59%[1]. |
体内活性 | ASK1-IN-2 (1 mg/kg; i.v.) shows low clearance (CL=1.38 L/h/kg) and moderate half-life (T1/2=1.45 h) in rats[1]. ASK1-IN-2 (10 mg/kg; p.o.) shows high oral exposure (AUClast=4517 h?ng/mL), 62.2% oral bioavailability and acceptable terminal half-life (T1/2=2.31 h) in rats[1]. ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) improves dextran sulphate sodium (DSS)-induced ulcerative colitis (UC) in mice[1]. ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) blocks ASK1-p38/JNK signaling pathways and reduces inflammatory cytokine levels in DSS-induced mouse colon tissues[1]. |
分子量 | 364.38 |
分子式 | C19H17FN6O |
CAS No. | 2541792-70-3 |
Smiles | CC(C)n1cnnc1-c1cccc(NC(=O)c2cc3ccc(F)cc3[nH]2)n1 |
密度 | 1.41 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: 249 mg/mL (683.35 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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