产品
编 号：F217186
分子式：C21H19FN8O2
分子量：434.43
分子式：C21H19FN8O2
分子量：434.43
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 1797432-62-2
产品详情
生物活性：
Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 (Tyk2) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a Ki value of 0.086 nM for Tyk2 JH2 and an IC50 value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis.
体内研究：
Tyk2-IN-5 (5、10 mg/kg；口服；每天两次，持续 20 天) 在大鼠辅助性关节炎模型中显示出高度有效性。 Tyk2-IN-5 (1，10 mg/kg；口服 single) 以剂量依赖性方式抑制 IL-12/IL-18 诱导的 IFNγ 产生。 Tyk2-IN-5 (10 mg/kg；口服；单次) 在大鼠中表现出高口服暴露和生物利用度 (114%)。Animal Model:Lewis male rats (rat adjuvant arthritis model).
Dosage:5, 10 mg/kg
Administration:Oral administration; twice daily for 20 days
Result:Demonstrated full efficacy to prevent the rats′ paw from swelling.
Animal Model:Lewis male rats (IL-12/IL-18-induced).
Dosage:1, 10 mg/kg
Administration:Oral administration; single
Result:Inhibited IL-12/IL-18 induced IFNγ production by 45% and 77% at doses of 1 and 10 mg/kg, respectively.
Animal Model:Lewis male rats, mouse.
Dosage:10 mg/kg
Administration:Oral administration; single
Result:1.19Pharmacokinetic Parameters of Tyk2-IN-5 in mouse and rat.PO (10 mg/kg)mouse rat
Cmax (μM)159.4
AUC0-24 (μM?h)1957
CL (mL/min/kg)167.8
F (%)86114
体外研究：
Tyk2-IN-5 以 >2 μM 的 IC50 值抑制 Jak1-3，并显示 IC50>12.5 μM 的 Jak1-3 依赖性细胞活性。
Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 (Tyk2) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a Ki value of 0.086 nM for Tyk2 JH2 and an IC50 value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis.
体内研究：
Tyk2-IN-5 (5、10 mg/kg；口服；每天两次，持续 20 天) 在大鼠辅助性关节炎模型中显示出高度有效性。 Tyk2-IN-5 (1，10 mg/kg；口服 single) 以剂量依赖性方式抑制 IL-12/IL-18 诱导的 IFNγ 产生。 Tyk2-IN-5 (10 mg/kg；口服；单次) 在大鼠中表现出高口服暴露和生物利用度 (114%)。Animal Model:Lewis male rats (rat adjuvant arthritis model).
Dosage:5, 10 mg/kg
Administration:Oral administration; twice daily for 20 days
Result:Demonstrated full efficacy to prevent the rats′ paw from swelling.
Animal Model:Lewis male rats (IL-12/IL-18-induced).
Dosage:1, 10 mg/kg
Administration:Oral administration; single
Result:Inhibited IL-12/IL-18 induced IFNγ production by 45% and 77% at doses of 1 and 10 mg/kg, respectively.
Animal Model:Lewis male rats, mouse.
Dosage:10 mg/kg
Administration:Oral administration; single
Result:1.19Pharmacokinetic Parameters of Tyk2-IN-5 in mouse and rat.PO (10 mg/kg)mouse rat
Cmax (μM)159.4
AUC0-24 (μM?h)1957
CL (mL/min/kg)167.8
F (%)86114
体外研究：
Tyk2-IN-5 以 >2 μM 的 IC50 值抑制 Jak1-3，并显示 IC50>12.5 μM 的 Jak1-3 依赖性细胞活性。
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