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TAK-715

TAK-715

产品编号 T6150   CAS 303162-79-0

TAK-715 是一种具有口服活性的p38 MAPK 抑制剂,对 p38α 和 p38β 的IC50分别为 7.1 nM 和200 nM。它抑制酪蛋白激酶 I (CK1δ/ε),调节 Wnt/β-catenin 信号传导的激活,有抗炎活性。

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TAK-715 Chemical Structure
TAK-715, CAS 303162-79-0
规格 价格/CNY 货期 数量
1 mg ¥ 285 现货
2 mg ¥ 419 现货
5 mg ¥ 689 现货
10 mg ¥ 980 现货
25 mg ¥ 1,680 现货
50 mg ¥ 2,530 现货
100 mg ¥ 3,730 现货
1 mL * 10 mM (in DMSO) ¥ 729 现货
产品目录号及名称: TAK-715 (T6150)
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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 TAK-715 is a p38 MAPK inhibitor for p38α.
靶点活性 p38β:0.20 μM, p38α:7.1 nM
体外活性 TAK 715 inhibits LPS-stimulated release of TNF-alpha from THP-1 with IC50 of 48 nM. [1] TAK 715 (10 μM) inhibits Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells. [2] The amide NH of TAK 715 is hydrogen bonded to the main-chain carbonyl of Met109 of p38 alpha. TAK 715 binds relatively high in the ATP pocket, occupying the hydrophobic back pocket, the adenine region and the front pocket of p38 as well as extending to most of the length of the Gly-rich loop. [3]
体内活性 TAK 715 (10 mg/kg, po) inhibits LPS-induced TNF-alpha production in mice with 87.6% inhibition. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 results in Cmax of 0.19 μg/mL and AUC(0-24 hours) of 1.16 μg·h/mL in rats. TAK 715 (30 mg/kg, po) significantly reduces the secondary paw volume with 25 % inhibition in a rat adjuvant-induced arthritis (AA) model. [1]
激酶实验 Assay of PI3K enzyme inhibition: The inhibition of PI3Kβ, PI3Kα, PI3Kγ, and PI3Kδ is evaluated in an AlphaScreen based enzyme activity assay using human recombinant enzymes. The assay measures PI3K-mediated conversion of PIP2 to PIP3. Biotinylated PIP3, a GST-tagged pleckstrin homology (PH) domain and the two AlphaScreen beads form a complex that elicits a signal upon laser excitation at 680 nm. The PIP3 formed in the enzyme reaction competes with the biotinylated PIP3 for binding to the PH domain thus reducing the signal with increasing enzyme product. The AZD6482 is dissolved in DMSO and added to 384 well plates. PBKβ, PBKα, PBKγ, or PBKδ is added in a Tris buffer (50 mM Tris pH 7.6, 0.05% CHAPS, 5 mM DTT, and 24 mM MgCl2) and allowed to preincubate with AZD6482 for 20 minutes prior to the addition of substrate solution containing PIP2 and ATP. The enzyme reaction is stopped after 20 minutes by addition of stop solution containing EDTA and biotin-PIP3, followed by addition of detection solution containing GST-grpl PH and AlphaScreen beads. Plates are left for a minimum of 5 hours in the dark prior to analysis. The final concentration of DMSO, ATP and PIP2 in the assay are, 0.8%, 4 μM, and 40 μM, respectively. IC50 values are calculated according to the equation, y = {a+[(b-a)/(l+(x/IC50)s)]}, where y = % inhibition; a = 0%; b = 100%; s = the slope of the concentration-response curve; x = AZD6482 concentration.
分子量 399.51
分子式 C24H21N3OS
CAS No. 303162-79-0

存储

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

溶解度

Ethanol: 20 mg/mL (50 mM)

DMSO: 40 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.5031 mL 12.5153 mL 25.0307 mL 62.5767 mL
5 mM 0.5006 mL 2.5031 mL 5.0061 mL 12.5153 mL
10 mM 0.2503 mL 1.2515 mL 2.5031 mL 6.2577 mL
20 mM 0.1252 mL 0.6258 mL 1.2515 mL 3.1288 mL
50 mM 0.0501 mL 0.2503 mL 0.5006 mL 1.2515 mL
DMSO 100 mM 0.025 mL 0.1252 mL 0.2503 mL 0.6258 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Miwatashi S, et al. J Med Chem, 2005, 48(19), 5966-5979. 2. Verkaar F, et al. Chem Biol, 2011, 18(4), 485-494. 3. Azevedo R, et al. Acta Crystallogr D Biol Crystallogr. 2012 Aug;68(Pt 8):1041-50.
CK1-IN-2 Silmitasertib sodium salt Ac-VDVAD-CHO PF-4800567 CKI-7 CK2 inhibitor 2 SSTC3 Casein kinase 1δ-IN-4

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 神经退行性疾病化合物库 抗癌药物库 抗糖尿病库 细胞骨架化合物库 抗衰老化合物库 MAPK 抑制剂库 药物功能重定位化合物库 神经再生化合物库 口服活性化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

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

TAK-715 303162-79-0 MAPK Metabolism Stem Cells p38 MAPK Casein Kinase JNK CYP3A4 MEKK1 orally ERK1 TAK715 IKKβ TNF-α CTGF Snai1 Inhibitor JNK1 Wnt/β-catenin TAK1 arthritis inhibit hDvl2 TAK 715 inhibitor

 

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