计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC 50 value of 0.19 nM and a K i 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 IC 50 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
In Vitro
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs. Potential advantages of deuterated compounds: (1) Extend the half-life in vivo. Deuterated compounds may be able to prolong the pharmacokinetic characteristics of the compound, that is, prolong the half-life in vivo. This can improve compound safety, efficacy and tolerability, and increase ease of administration. (2) Improve oral bioavailability. Deuterated compounds may reduce the degree of unwanted metabolism (first-pass metabolism) in the gut wall and liver, allowing a greater proportion of the unmetabolized drug to reach its target site of action. High bioavailability determines its activity at low doses and better tolerance. (3) Improve metabolic characteristics. Deuterated compounds may reduce the formation of toxic or reactive metabolites and improve drug metabolism. (4) Improve drug safety. Deuterated compounds may reduce or eliminate adverse side effects of pharmaceutical compounds and are safe. (5) Preserve the therapeutic properties. Deuterated compounds are expected to retain similar biochemical potency and selectivity to hydrogen analogs in previous studies. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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% . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.
IC50& Target:Tyk2 JH2 0.19 nM (IC 50 ) Tyk2 JH2 0.02 nM (Ki) CYP2C19 14 μM (IC 50 )
规格
规格或纯度
10mM in DMSO
英文名称
BMS-986202
生化机理
BMS-986202 是一种强效、选择性和口服活性 Tyk2 抑制剂，它能与 Tyk2 JH2 结合，IC 50 值为 0.19 nM，K i 为 0.02 nM。BMS-986202 对包括 Jak 家族成员在内的其他激酶具有显著的选择性。BMS-986202 对其他激酶（包括 Jak 家族成员）也有很强的选择性。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
[2H]C([2H])([2H])NC(=O)C1=CN=C(C=C1NC2=CC=CC(=C2OC)C3=NC=C(C=N3)F)NC(=O)C4CC4
关联CAS
PubChem CID
MeSH Entry Terms
1-(4-(4-(3-methyl-4-((((1R)-1-phenylethoxy)carbonyl)amino)-1,2-oxazol-5-yl)phenyl)phenyl)cyclopropane-1-carboxylic acid;BMS-986202
分子量
439.46
技术文档
高级数据
关联靶点（人）
TYK2
Tclin
非受体酪氨酸蛋白激酶 TYK2(Non-receptor tyrosine-protein kinase TYK2)
(4 活性数据)
JAK1
Tclin
酪氨酸蛋白激酶JAK1(Tyrosine-protein kinase JAK1)
(1 活性数据)
安全和危险性（GHS）
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
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