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Ki16425

Ki16425

产品编号 T6108   CAS 355025-24-0
别名: Debio 0719

Ki16425 (Debio 0719) 是一种竞争性、有效和可逆的 LPA1、LPA2 和 LPA3 拮抗剂,Ki 分别为 0.34、6.5 和 0.93 μM。它可抑制LPA 诱导的 HEK293A 细胞中 YAP/TAZ 的去磷酸化,降低LPA 诱导的 p42/p44 MAPK 激活。

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Ki16425 Chemical Structure
Ki16425, CAS 355025-24-0
规格 价格/CNY 货期 数量
1 mg ¥ 293 现货
2 mg ¥ 413 现货
5 mg ¥ 672 现货
10 mg ¥ 987 现货
25 mg ¥ 1,830 现货
50 mg ¥ 2,730 现货
100 mg ¥ 3,920 现货
1 mL * 10 mM (in DMSO) ¥ 736 现货
产品目录号及名称: Ki16425 (T6108)
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纯度: 96.15%
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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 Ki16425 (Debio 0719) is a competitive, potent and reversible antagonist to LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM, respectively.
靶点活性 LPA2:6.5 μM(Ki), LPA1:0.34 μM(Ki), LPA3:0.93 μM(Ki)
体外活性 Kil6425 preferentially inhibits LPA1- and LPA3-mediated responses but has only a moderate effect on LPA2. Ki16425 inhibits the LPA-induced Ca(2+) response in THP-1 cells, 3T3 fibroblasts, and A431 cells, but had only a marginal effect in PC-12 cells and HL-60 cells, which means that Ki16425 seems to be a useful tool for evaluating the involvement of specific LPA receptors in the short-term response to LPA. Ki16425 inhibits long-term DNA synthesis and cell migration as induced by LPA in Swiss 3T3 fibroblasts. [1] Ki16425 reduces the LPA-induced activation of p42/p44 mitogen activated protein kinase (MAPK), while acting as a weak stimulator of p42/p44 MAPK on its own, properties typical of a protean agonist. Ki16425 also significantly reduces the NGF-induced stimulation of p42/p44 MAPK and inhibited NGF-stimulated neurite outgrowth in PC-12 cells. [2] Ki16425 markedly inhibits the expressions of COX-2 protein induced by synovial fluids. The enhancement of the IL-1 action by LPA on COX-2 expression is also inhibited by Ki16425. [3]
体内活性 Ki-16425 (30 mg/kg, i.p.) completely blocks LPA-induced neuropathic pain-like behaviors, when administered 30 min but not 90 min before lysophosphatidic acid injection, suggesting that Ki-16425 is a short-lived inhibitor. Ki-16425 also inhibits nerve injury-induced up-regulation of Caα2δ-1 in the dorsal root ganglion and reduction of SP immunoreactivity in the spinal dorsal horn. [4]
激酶实验 High-throughput screening: Screening is conducted at the ICCB-Longwood screening facility. 10 μL of recombinant USP14 protein are dispensed into each well of a 384-well low volume plate in duplicate, using a Wellmate plate dispenser. 33.3?nL of compound from the library are pin-transferred into the wells using a Seiko pin transfer robotic system, followed by pre-incubation for about 30?min. The last two columns of each plate are used for positive and negative controls for the assay. To initiate the enzyme reaction, 10?μL of VS-proteasome plus Ub-AMC mixture are added to each well, using a Wellmate dispenser. Samples are then incubated for another 45?min. Ub-AMC hydrolysis is measured at Ex355/Em460 using an Envision plate reader. The final concentrations of USP14, VS-proteasome and Ub-AMC are 15?nM, 1?nM and 0.8 μM, respectively. The final concentration of test compound is approximately 17?μM. Enzymes and substrates are prepared in Ub-AMC assay buffer (50?mM Tris-HCl (pH?7.5), 1?mM EDTA, 1?mM ATP, 5 mM MgCl2, 1?mM DTT, and 1 mg/Ml ovalbumin).
别名 Debio 0719
分子量 474.96
分子式 C23H23ClN2O5S
CAS No. 355025-24-0

存储

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

溶解度

DMSO: 94 mg/mL (197.91 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 84 mg/mL(176.9 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 2.1054 mL 10.5272 mL 21.0544 mL 52.636 mL
5 mM 0.4211 mL 2.1054 mL 4.2109 mL 10.5272 mL
10 mM 0.2105 mL 1.0527 mL 2.1054 mL 5.2636 mL
20 mM 0.1053 mL 0.5264 mL 1.0527 mL 2.6318 mL
50 mM 0.0421 mL 0.2105 mL 0.4211 mL 1.0527 mL
100 mM 0.0211 mL 0.1053 mL 0.2105 mL 0.5264 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. Ohta H, et al, Mol Pharmacol, 2003, 64(4), 1994-12005. 2. Moughal NA, et al. J Neurochem, 2006, 98(6), 1920-1929. 3. Nochi H, et al. J Immunol, 2008, 181(7), 5111-5119. 4. Ma L, et al. J Neurochem, 2009, 109(2), 603-610.
BMS-986278 Ki16198 GRI977143 1-Oleoyl lysophosphatidic acid sodium AM095 Edg-2 receptor inhibitor 1 AM095 free acid LX-1031

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 经典已知活性库 临床前化合物库 抑制剂库 已知活性化合物库 GPCR靶点分子库 ReFRAME 相关化合物库 抗纤维化化合物库 抗癌化合物库 NO PAINS 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

Ki16425 355025-24-0 GPCR/G Protein LPA Receptor LPL Receptor Lysophospholipid Receptor Inhibitor Debio0719 Ki-16425 inhibit Debio-0719 Ki 16425 Debio 0719 inhibitor

 

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