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MD2-IN-1

MD2-IN-1

产品编号 T4231   CAS 111797-22-9

MD2-IN-1 是骨髓分化蛋白 2 (MD2) 的抑制剂,对重组人 MD2 (rhMD2) 的 KD 为 189  μM。

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MD2-IN-1 Chemical Structure
MD2-IN-1, CAS 111797-22-9
规格 价格/CNY 货期 数量
1 mg ¥ 632 现货
5 mg ¥ 1,830 现货
10 mg ¥ 2,930 现货
25 mg ¥ 4,880 现货
50 mg ¥ 6,950 现货
100 mg ¥ 9,390 现货
1 mL * 10 mM (in DMSO) ¥ 1,950 现货
产品目录号及名称: MD2-IN-1 (T4231)
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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 MD2-IN-1 is a Myeloid differentiation protein 2 (MD2) inhibitor with a KD of 189  μM for the recombinant human MD2 (rhMD2).
靶点活性 rhMD2:189 μM (KD)
体外活性 Pre-treatment with different doses of MD2-IN-1 dose-dependently reduces FITC-LPS binding to MD2 in cell surface membranes, with a 65% inhibition at 10?μM in terms of mean fluorescence intensity. Pretreatment with MD2-IN-1 also dose-dependently blocks LPS-induced MAPK phosphorylation in the MPMs. Compared to the vehicle, LPS alone largely increases the amount of TLR4/MD2 complex, while pretreatment with MD2-IN-1 inhibits the increase of TLR4/MD2 complex to the vehicle level. SPR analysis shows that MD2-IN-1 exhibits recognizable binding to rhMD2 protein in a dose-dependent manner, with a KD value of 189?μM, while the KD value of xanthohumol binding to MD2 is 460?μM.
体内活性 The lung wet/dry weight ratio is markedly higher in the LPS-treated group compared to controls, and MD2-IN-1 treatment reduces LPS-induced pulmonary edema. Administration of MD2-IN-1 evidently reduces the LPS-induced increase in protein concentrations in BALF. LPS also causes observable lung histopathologic changes, including areas of inflammatory infiltration, hemorrhage, interstitial edema, thickening of the alveolar wall, and lung tissue destruction. These histopathological changes are ameliorated in the MD2-IN-1 treatment group.
细胞实验 Mouse RAW264.7 macrophages are starved for 3?h before experimentation. Cells are incubated with or without FITC-LPS (50?μg/mL) in the presence or absence of MD2-IN-1 (0.1, 1 and 10?μM) for 30?min. After incubation, macrophages are fixed with paraformaldehyde for 10?min at 4°C and washed with PBS before being analyzed by flow cytometry.
动物实验 Male Sprague Dawley (SD) rats are randomly divided into three groups,designated "control" (5 rats,only receive the vehicle of 0.9% saline),"LPS" (7 rats,receive 5?mg/kg LPS alone) and "MD2-IN-1 (20)?+?LPS" (6 rats,receive both MD2-IN-1 and 5?mg/kg LPS).Prior to LPS-induced Acute lung injury (ALI),the MD2-IN-1+LPS group rats are treated intragastrically with MD2-IN-1 at a dosage of 20?mg/kg/day continuously for one week.Under ether anesthesia,all the rats are exposed their trachea and challenged with intratracheal instillation of 50?μL of LPS,while the control group challenged with intratracheal instillation of 50?μL of 0.9% saline.Rats are then euthanized with ketamine after 6?h of LPS induction.
分子量 358.39
分子式 C20H22O6
CAS No. 111797-22-9

存储

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

溶解度

DMSO: 55 mg/mL (153.46 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 1 mM 2.7903 mL 13.9513 mL 27.9026 mL 69.7564 mL
5 mM 0.5581 mL 2.7903 mL 5.5805 mL 13.9513 mL
10 mM 0.279 mL 1.3951 mL 2.7903 mL 6.9756 mL
20 mM 0.1395 mL 0.6976 mL 1.3951 mL 3.4878 mL
50 mM 0.0558 mL 0.279 mL 0.5581 mL 1.3951 mL
100 mM 0.0279 mL 0.1395 mL 0.279 mL 0.6976 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. Zhang Y, et al. Discovery of new MD2 inhibitor from chalcone derivatives with anti-inflammatory effects in LPS-induced acute lung injury. Sci Rep. 2016 Apr 27;6:25130.
RS 09 CU-CPT9b TLR7 agonist 2 RS09 2TFA (1449566-36-2 free base) TH1020 Isofraxidin Corilagin Polyinosinic-polycytidylic acid sodium

相关化合物库

该产品包含在如下化合物库中:
已知活性化合物库 经典已知活性库 HIF-1化合物库 抑制剂库 肿瘤免疫治疗小分子化合物库 细胞焦亡化合物库 免疫/炎症分子化合物库 非甾体类抗炎化合物库 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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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

MD2-IN-1 111797-22-9 Immunology/Inflammation TLR inhibit Inhibitor MD2IN1 Toll-like Receptor (TLR) MD-2-IN-1 MD2 IN 1 inhibitor

 

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