Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 94 mg/mL (197.91 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 84 mg/mL(176.9 mM)
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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