| Bioactivity | JAK3 covalent inhibitor-2 (compound J1b) is a selective, orally potent JAK3 inhibitor (IC50=7.2 nM) with low toxicity, anti-inflammatory activity and good bioavailability[1]. |
| Invitro | 细胞毒性试验：JAK3 covalent inhibitor-2 对 HEK293, LO2, 软骨细胞和 RAW264.7 的细胞毒性较低，IC50 (72 h) 分别为 86.82 μM (HEK293), 61.79 μM (LO2), >32 μM (软骨细胞)和 >32 μM (RAW264.7)[1]。代谢稳定性研究：JAK3 covalent inhibitor-2 (100 mM; 90 min) 在人和大鼠肝微粒体的 t1/2 分别是 13.1 min 和 43.9 min 。清除率分别为 132.5 mL/min/kg 和 132.5 mL/min/kg [1]。JAK3 covalent inhibitor-2 (0.125-8 μM; 48 h) 呈剂量依赖性诱导 T 淋巴细胞凋亡[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> JAK3 covalent inhibitor-2 相关抗体: Apoptosis Analysis[1] Cell Line: |
| In Vivo | 抗炎活性：JAK3 covalent inhibitor-2 (30 mg/kg; p.o.; 单剂量) 在 Carrageenan (HY-125474) 诱导的 ICR 小鼠足部水肿模型中，抑制水肿部位的厚度增加[1]。毒性实验: JAK3 covalent inhibitor-2 (2 g/kg, p.o.; 单剂量) 肝脏和肾脏似乎与正常小鼠相似,没有观察到体重损失或其他不良反应[1]。药代动力学: JAK3 covalent inhibitor-2 (5 mg/kg, p.o.) 清除率 (Cl) 为 7.37 l/h/kg, 口服半衰期 (t1/2 = 3.77 h), 和生物利用度 (F = 31.69%)[1]。Pharmacokinetic parameters of compound JAK3 covalent inhibitor-2 in SD rats[1] JAK3 covalent inhibitor-2 在SD大鼠体内的药代动力学分析[1] Route |
| CAS | 2664050-97-7 |
| Formula | C20H20N6O3 |
| Molar Mass | 392.41 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Hualiang Y et al. Design and synthesis of highly selective Janus kinase 3 covalent inhibitors for the treatment of rheumatoid arthritis ARCH PHARM. 2024 Feb e2300753 |
JAK3 covalent inhibitor-2
CAS: 2664050-97-7 F: C20H20N6O3 W: 392.41
JAK3 covalent inhibitor-2 (compound J1b) is a selective, orally potent JAK3 inhibitor (IC50=7.2 nM) with low toxicity, a
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