产品
编 号：F762095
分子式：C22H18D3FN6O3
分子量：439.46
分子式：C22H18D3FN6O3
分子量：439.46
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
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询价
结构图
CAS No: 1771691-34-9
产品详情
生物活性：
BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 value of 0.19 nM and a Ki of 0.02 nM. BMS-986202 is remarkably selective over other kinases including Jak family members. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 value of 14 μM. BMS-986202 can be used for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus research. BMS-986202 is a de novo deuterium.
体内研究：
BMS-986202 (Compound 7; 3-30 mg/kg; p.o.; daily; for 9 days) treatment inhibits IL-23-driven acanthosis in mice.BMS-986202 (Compound 7; 0.4-10 mg/kg; p.o.) treatment inhibits IL-12/IL-18-induced IFNγ production in mice. BMS-986202 dose-dependently inhibits IFNγ production by 46% and 80% at doses of 2 mg/kg and 10 mg/kg, respectively.BMS-986202 (Compound 7; 7-10 mg/kg; p.o.) is stable in liver microsomes, with half lives of greater than 120 min in mouse, rat, monkey, and humans and 89 min in dog. The serum protein binding for BMS-986202 in these species ranges from 89.3% to 96.0%, leaving a good range of free fraction of drug available. BMS-986202 shows the oral bioavailability up to 62-100%.Animal Model:C57BL/6 female mice (9-11 weeks) injected with IL-23
Dosage:3 mg/kg, 10 mg/kg, and 30 mg/kg
Administration:Oral administration; daily; for 9 days
Result:Inhibited ear swelling in a dose-responsive manner in IL-23-induced acanthosis in mice.
体外研究：
氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱。氘代化合物的潜在优势：（1）延长体内半衰期。氘代化合物或能够延长化合物的药代动力学特征，即延长体内半衰期。由此可提高化合物安全性、有效性和耐受性，并增加给药的便捷性。（2）提高口服生物利用度。氘代化合物或能够减少肠壁和肝脏中不需要的代谢 (首过代谢) 程度，使得更大比例的未代谢药物到达作用的目标位置。生物利用度高决定其在低剂量下具有活性以及更好的耐受性。（3）改善代谢特征。氘代化合物或能够减少有毒或反应性代谢物的形成，改善药物代谢状况。（4）改进药品安全性。氘代化合物或能够减少或消除药物化合物的不良副作用，具有安全性。（5）保留治疗特性。氘代化合物有望保留和此前研究中氢类似物相似的生化效力和选择性。
BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 value of 0.19 nM and a Ki of 0.02 nM. BMS-986202 is remarkably selective over other kinases including Jak family members. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 value of 14 μM. BMS-986202 can be used for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus research. BMS-986202 is a de novo deuterium.
体内研究：
BMS-986202 (Compound 7; 3-30 mg/kg; p.o.; daily; for 9 days) treatment inhibits IL-23-driven acanthosis in mice.BMS-986202 (Compound 7; 0.4-10 mg/kg; p.o.) treatment inhibits IL-12/IL-18-induced IFNγ production in mice. BMS-986202 dose-dependently inhibits IFNγ production by 46% and 80% at doses of 2 mg/kg and 10 mg/kg, respectively.BMS-986202 (Compound 7; 7-10 mg/kg; p.o.) is stable in liver microsomes, with half lives of greater than 120 min in mouse, rat, monkey, and humans and 89 min in dog. The serum protein binding for BMS-986202 in these species ranges from 89.3% to 96.0%, leaving a good range of free fraction of drug available. BMS-986202 shows the oral bioavailability up to 62-100%.Animal Model:C57BL/6 female mice (9-11 weeks) injected with IL-23
Dosage:3 mg/kg, 10 mg/kg, and 30 mg/kg
Administration:Oral administration; daily; for 9 days
Result:Inhibited ear swelling in a dose-responsive manner in IL-23-induced acanthosis in mice.
体外研究：
氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱。氘代化合物的潜在优势：（1）延长体内半衰期。氘代化合物或能够延长化合物的药代动力学特征，即延长体内半衰期。由此可提高化合物安全性、有效性和耐受性，并增加给药的便捷性。（2）提高口服生物利用度。氘代化合物或能够减少肠壁和肝脏中不需要的代谢 (首过代谢) 程度，使得更大比例的未代谢药物到达作用的目标位置。生物利用度高决定其在低剂量下具有活性以及更好的耐受性。（3）改善代谢特征。氘代化合物或能够减少有毒或反应性代谢物的形成，改善药物代谢状况。（4）改进药品安全性。氘代化合物或能够减少或消除药物化合物的不良副作用，具有安全性。（5）保留治疗特性。氘代化合物有望保留和此前研究中氢类似物相似的生化效力和选择性。
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