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Upadacitinib (ABT-494) 是高效选择性的,具有口服活性的 JAK1抑制剂,IC50为43 nM,可用于多种自身免疫性疾病的研究。它对 JAK1 的选择性约为 JAK2 的 74 倍。
Upadacitinib (ABT-494) 是高效选择性的,具有口服活性的 JAK1抑制剂,IC50为43 nM,可用于多种自身免疫性疾病的研究。它对 JAK1 的选择性约为 JAK2 的 74 倍。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 333 | 现货 | |
2 mg | ¥ 482 | 现货 | |
5 mg | ¥ 777 | 现货 | |
10 mg | ¥ 1,160 | 现货 | |
25 mg | ¥ 2,430 | 现货 | |
50 mg | ¥ 3,550 | 现货 | |
100 mg | ¥ 5,130 | 现货 | |
200 mg | ¥ 6,920 | 现货 | |
500 mg | ¥ 9,870 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 659 | 现货 |
产品描述 | Upadacitinib (ABT-494) (ABT-494) is a selective Janus kinase (JAK) 1 inhibitor, which is being studied for the treatment of several autoimmune disorders in the IC50 of 43 nM. |
靶点活性 | JAK2:200 nM, JAK1:43 nM |
体外活性 | Upadacitinib is 74-fold more selective for JAK-1 than for JAK-2, which is involved in erythropoiesis. And Upadacitinib is 58-fold more selective for JAK-1 than for JAK-3, which is involved in immunosurveillance. The enhanced selectivity of Upadacitinib for JAK-1 over JAK-2 and JAK-3 may offer an improved benefit-risk profile in patients with RA range. |
体内活性 | Upadacitinib, a second JAK inhibitor, has been developed by AbbVie.Upadacitinib finished multiple-dose Phase I studies in 2013. Upadacitinib show to be safe and well-tolerated up to multiple doses of 24 mg twice daily using the immediate release formulation in phase I trials. Upadacitinib exposure is dose proportional to the evaluated multiple dose. |
别名 | 乌帕替尼, ABT-494 |
分子量 | 380.37 |
分子式 | C17H19F3N6O |
CAS No. | 1310726-60-3 |
Smiles | CC[C@@H]1CN(C[C@@H]1c1cnc2cnc3[nH]ccc3n12)C(=O)NCC(F)(F)F |
密度 | 1.56 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: 55 mg/mL (144.6 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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