化合物MD2-IN-1 T4231

Product Introduction
Bioactivity


英文名: MD2-IN-1

描述: 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。

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.

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.

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

溶解度: DMSO : 55 mg/mL (153.46 mM)


关键字: inhibit | MD2-IN-1 | Inhibitor | MD2IN1 | Toll-like Receptor (TLR) | MD-2-IN-1 | MD2 IN 1

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相关库: HIF-1 Signaling Pathway Compound Library | Pyroptosis Compound Library | Immuno-Oncology Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | NO PAINS Compound Library | Nonsteroidal Anti-Inflammatory Compound Library | Bioactive Compound Library

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