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SAR-20347

SAR-20347

产品编号 T4210   CAS 1450881-55-6
别名: SAR20347

SAR-20347 是 TYK2、JAK1、JAK2和JAK3的抑制剂,IC50值分别为 0.6、23、26 和 41 nM。

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SAR-20347 Chemical Structure
SAR-20347, CAS 1450881-55-6
规格 价格/CNY 货期 数量
1 mg ¥ 413 现货
2 mg ¥ 598 现货
5 mg ¥ 970 现货
10 mg ¥ 1,680 现货
25 mg ¥ 3,660 现货
50 mg ¥ 5,330 现货
100 mg ¥ 7,520 现货
500 mg ¥ 14,800 现货
1 mL * 10 mM (in DMSO) ¥ 1,090 现货
千万补贴 助力科研
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产品目录号及名称: SAR-20347 (T4210)
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纯度: 99.77%
纯度: 99.54%
纯度: 99.35%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 SAR-20347 is an inhibitor of TYK2, JAK1/2/3 (IC50: 0.6/23/26/41 nM).
靶点活性 JAK2:26nM, JAK1:23nM, TYK2:0.6 nM, JAK3:41 nM
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 Compared to vehicle-treated animals, SAR-20347 (60 mg/kg) inhibits the production of IFN-γ in the serum by 91%, demonstrating that SAR-20347 can inhibit TYK2 signaling in vivo. SAR-20347 markedly reduces IL-17 production as measured by average signal intensity, consistent with the gene expression analysis.
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].
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].
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].
别名 SAR20347
分子量 444.84
分子式 C21H18ClFN4O4
CAS No. 1450881-55-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 100 mg/mL

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TargetMol Library Books参考文献

1. Works MG, et al. Inhibition of TYK2 and JAK1 ameliorates imiquimod-induced psoriasis-like dermatitis by inhibiting IL-22 and the IL-23/IL-17 axis. J Immunol. 2014 Oct 1;193(7):3278-87. 2. Kang X, Yang M, Shi Y, et al. Interleukin-15 facilitates muscle regeneration through modulation of fibro/adipogenic progenitors[J]. Cell Communication and Signaling. 2018 Jul 20;16(1):42.

TargetMol Library Books文献引用

1. Kang X, Yang M, Shi Y, et al. Interleukin-15 facilitates muscle regeneration through modulation of fibro/adipogenic progenitors. Cell Communication and Signaling. 2018 Jul 20;16(1):42 2. Zhang X, Wang J, Wang M, et al.IFN-β Pretreatment Alleviates Allogeneic Renal Tubular Epithelial Cell–Induced NK Cell Responses via the IRF7/HLA-E/NKG2A Axis.The Journal of Immunology.2023
Ruxolitinib Ginsenoside Ra1 Tyrphostin AG30 Beta-Hydroxyisovalerylshikonin JAK-IN-21 Zongertinib Paltimatrectinib GSK 3 Inhibitor IX

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 酪氨酸激酶分子库 表观遗传库 血液病分子库 激酶抑制剂库 抗肝癌化合物库 细胞重编程化合物库 干细胞分化化合物库 已知活性化合物库 血管生成库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

SAR-20347 1450881-55-6 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors Tyrosine Kinases JAK inhibit Janus kinase SAR20347 SAR 20347 Inhibitor inhibitor

 

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