化合物SAR20347 T4210
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
50 mg | 1450881-55-6 | ¥5,330.00 | 询底价 |
25 mg | 1450881-55-6 | ¥3,660.00 | 询底价 |
5 mg | 1450881-55-6 | ¥970.00 | 询底价 |
1 mL | 1450881-55-6 | ¥1,090.00 | 询底价 |
100 mg | 1450881-55-6 | ¥7,520.00 | 询底价 |
1 mg | 1450881-55-6 | ¥413.00 | 询底价 |
500 mg | 1450881-55-6 | ¥14,800.00 | 询底价 |
2 mg | 1450881-55-6 | ¥598.00 | 询底价 |
10 mg | 1450881-55-6 | ¥1,680.00 | 询底价 |
Product Introduction
Bioactivity
英文名: SAR-20347
描述: SAR-20347 是 TYK2、JAK1、JAK2和JAK3的抑制剂,IC50值分别为 0.6、23、26 和 41 nM。
细胞实验: Cells are plated in a 96-well v-bottom plate in starvation medium, incubated with SAR-20347 (0.5% DMSO) for 20 minutes at 37°C, 5% CO2, and stimulated with individual cytokines. P-STAT levels are measured in duplicate using MSD plates following the manufacturer's instructions (MSD)[1].
激酶实验: Kinases are prepared in Base Reaction Buffer (20 mM Hepes pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, 1% DMSO) and substrate is added with 1.5 mM CaCl2, 16 μg/mL Calmodulin, and 2 mM MnCl2. Varying concentrations of SAR-20347 in DMSO are added to the kinase reaction along with 10 μM 33P-ATP (activity 0.01 μCi/μL final) for IC50 determination[1].
动物实验: Female 7 to 9-week old C57BL/6 mice are used. Mice are administered vehicle or 50 mg/kg SAR-20347 by oral gavage 30 minutes prior to application of 62.5 mg 5% imiquimod cream or control cream. Another dose of vehicle or 50 mg/kg SAR-20347 is given 5.5 hours following the first dose. This treatment is repeated for 5 days and on day 3 and 4, animals are injected with 100 uL saline to prevent dehydration. On the 6th day, the animals are euthanized and photographs are taken[1].
体外活性: SAR-20347 effectively inhibits IL-12-mediated STAT4 phosphorylation (TYK2-dependent, IC50: 126 nM) when NK-92 cells are stimulated with IL-12. In the culture media, cells without IL-12 have no measurable IFN-γ, while cells incubated with IL-12 and SAR-20347 demonstrate dose-dependent inhibition of IFN-γ production. SAR-20347 (maximum effect: 5 μM) dose-dependently inhibits the production of secreted embryonic alkaline phosphatase (SEAP).
体内活性: 与对照组动物相比,SAR-20347(60 mg/kg)能够在体内抑制TYK2信号传导,表现为抑制血清中IFN-γ的产量达91%。此外,通过平均信号强度的测量,SAR-20347显著减少了IL-17的产生,这与基因表达分析的结果是一致的。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 55 mg/mL (123.64 mM)
关键字: inhibit | Janus kinase | JAK | SAR 20347 | SAR-20347 | Inhibitor
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相关库: Anti-Aging Compound Library | Anti-Liver Cancer Compound Library | Anti-Cancer Compound Library | Angiogenesis related Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Kinase Inhibitor Library | Inhibitor Library | Tyrosine Kinase Inhibitor Library | Reprogramming Compound Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途