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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1797432-62-2
- 规格：
10 mM * 1 mL/1 mg/5 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥4950.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥2045.0 |
| 规格： | 5 mg | 产品价格： | ￥4500.0 |
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Tyk2-IN-5
CAS No. : 1797432-62-2
MCE 国际站：Tyk2-IN-5
产品活性：Tyk2-IN-5 (compound 6) 是一种强效的、具有选择性和口服活性的酪氨酸激酶 2 (Tyk2) 抑制剂，作用于 JH2 结构域。Tyk2-IN-5 对 Tyk2 JH2 的 Ki 值为 0.086 nM，对 IFNα 的 IC50 值为 25 nM。Tyk2-IN-5 能高效地抑制药效学大鼠模型中 IFNγ 的产生，对大鼠关节炎模型具有完全的疗效。
研究领域：Epigenetics | Protein Tyrosine Kinase/RTK | JAK/STAT Signaling | Stem Cell/Wnt
作用靶点：JAK
In Vitro: Tyk2-IN-5 inhibits Jak1-3 with IC50 values of >2 μM and displays the Jak1-3 dependent cellular activities of >12.5 μM (IC50 values).
In Vivo: Tyk2-IN-5 (5, 10 mg/kg; p.o.; twice daily for 20 days) shows highly efficacious in a rat adjuvant arthritis model.
?Tyk2-IN-5 (1, 10 mg/kg; p.o.; single) inhibits IL-12/IL-18 induced IFNγ production in a dose-dependent manner.
?Tyk2-IN-5 (10 mg/kg; p.o.; single) shows a high oral exposure and bioavailability (114%) in rat.
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文献和实验参数 动物种胆红素 mg%胆固醇 mg%肌酐 mg%葡萄糖 mg%尿素氮 mg%尿酸 mg%钠 mEg/l钾 mEg/l氯 mEg/l重碳酸盐 mEg/l无机磷 mg%钙 mg%镁 mg%小鼠0.75±0.050.60±0.04(0.10-0.90)63.3±11.865.5±21.1(26.0-82.4)0.84±0.190.67±0.17(0.30-1.00)92.2±10.585.0±9.50(62.8-176)20.8±5.8617.9±4.50(13.9-28.3)4.12±
Isolation Kit CD5(Ly-1) MicroBeadsCD8a(Ly-2) MicroBeadsCD8a+ T Cell Isolation Kit CD25 MicroBead KitCD62L(L-selectin) MicroBeadsAnti-MHC class II MicroBeadsCD4-FITC/PE/APCCD8a-FITC/PE/APCCD25-PECD62L-FITC/PE/APCCD90-FITC/PE/APC细胞因子分泌细胞Mouse IFN-r Secretion
AST U/L 34.78±10.70 276 6.07-62.75
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