2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  3. JAK Apoptosis
  4. JAK3 covalent inhibitor-2

JAK3 covalent inhibitor-2 (compound J1b) 是一种选择性、口服有效的 JAK3 抑制剂 (IC50=7.2 nM)，具有低毒性、抗炎活性和良好的生物利用度。

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JAK3 covalent inhibitor-2 Chemical Structure

JAK3 covalent inhibitor-2 Chemical Structure

CAS No. : 2664050-97-7

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JAK3 covalent inhibitor-2 相关抗体

Top Publications Citing Use of Products

查看 JAK 亚型特异性产品:

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JAK1 JAK2 JAK3 Tyk2 JAK

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target[1]

JAK3

7.2 nM (IC50)

体外研究
(In Vitro)

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.

JAK3 covalent inhibitor-2 相关抗体:

Apoptosis Analysis[1]

Cell Line: CD4+ T cells , CD8[1] T cells
Concentration: 0.125, 0.5, 1, 2, 4, 8 μM
Incubation Time: 48 h
Result: Dose-dependently led to apoptosis among CD4+ and CD8+ T cells
体内研究
(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 Dose (mg/kg) Cmax (mg/L) tmax (h) t1/2 (h) AUC0-t (mg/L·h) V<, V/F (L/kg) Cl, Cl/F (L/h/kg) F (%)
i.v. 5 4497.32 0.08 2.63 2161.38 8.98 (V) 2.32V (Cl) 31.69
p.o. 5 501.8 0.25 3.77 684.87 39.89 (V/F) 7.37 (Cl/F) /

治疗关节炎实验： JAK3 covalent inhibitor-2 ( 60 mg/kg; p.o.; 一天一次)，在胶原蛋白诱导的关节炎 (CIA) 模型中，几乎完全恢复了正常的关节状态，而且没有观察到明显的体重变化或其他不良反应[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ICR mice [1]
Dosage: 30 mg/kg
Administration: p.o.
Result: Showed significant anti-inflammatory activity by oral administration.
Animal Model: C57BL/6 mice[1]
Dosage: 2 g/kg
Administration: p.o.
Result: Inhibited tumor growth. Livers and kidneys appeared to be similar to those of normal mice. No weight loss or other adverse effects were observed.
Animal Model: SD rats[1]
Dosage: 5 mg/kg
Administration: p.o
Result: JAK3 covalent inhibitor-2 had good intestinal absorption and oral bioavailability. Clearance rate (Cl) was 7.37 L/h/kg, oral half‐life (t1/2 = 3.77 h), F = 31.69%
Animal Model: CIA model mouse[1]
Dosage: JAK3 covalent inhibitor-2 (30 mg/kg), JAK3 covalent inhibitor-2 (60 mg/kg,) Tofacitinib（HY-40354） (30 mg/kg)
Administration: p.o.
Result: JAK3 covalent inhibitor-2 group at 60 mg/kg histopathological analysis showed that the joint had returned to almost normal conditions.
分子量

392.41

Formula

C20H20N6O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

JAK3 covalent inhibitor-2 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JAK3 covalent inhibitor-22664050-97-7JAKApoptosisJanus kinasecovalent inhibitorsJAK3rheumatoid arthritisselectivity，systemic immunosuppressionCIAInhibitorinhibitorinhibit

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