乌帕替尼 T7503

Product Introduction
Bioactivity


英文名: Upadacitinib

描述: 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。

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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 55 mg/mL (144.6 mM)


关键字: ABT 494 | inhibit | Inhibitor | autoimmune | Upadacitinib | orally active | JAK | JAK1 | Janus kinase | ABT494

相关产品: Oclacitinib maleate | SB1317 hydrochloride (1204918-72-8(free base)) | SAR-20347 | JAK3i | STAT3-IN-18 | Degrasyn | Mollugin | FLLL32 | JAK1-IN-4 | WP1066

相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Highly Selective Inhibitor Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Anti-Pancreatic Cancer Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途