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111797-22-9

中文名稱 MD2-IN-1
英文名稱 MD2-IN-1
CAS 111797-22-9
分子式 C20H22O6
分子量 358.39
MOL 文件 111797-22-9.mol
更新日期 2023/07/03 08:46:51
111797-22-9 結(jié)構(gòu)式 111797-22-9 結(jié)構(gòu)式

基本信息

中文別名
化合物MD2-IN-1
英文別名
MDK7229
MDK 7229
MD2-IN-1
MD2 inhibitor 1
MD2-IN-1
MDK7229
MDK 7229
MDK 7229
2-Propen-1-one, 1-(3,4-dimethoxyphenyl)-3-(3,4,5-trimethoxyphenyl)-

物理化學(xué)性質(zhì)

熔點(diǎn)131-132 °C
沸點(diǎn)521.3±50.0 °C(Predicted)
密度1.156±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO : 50 mg/mL (139.51 mM);Water : < 0.1 mg/mL (insoluble)
形態(tài)Solid
顏色Light yellow to yellow

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
防范說(shuō)明P261-P305+P351+P338
MD2-IN-1價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-103483MD2-IN-1
MD2-IN-1
111797-22-91mg800元
2024/11/08HY-103483MD2-IN-1
MD2-IN-1
111797-22-95mg1600元
2024/11/08HY-103483MD2-IN-1
MD2-IN-1
111797-22-910mM * 1mLin DMSO1760元

常見問(wèn)題列表

生物活性
MD2-IN-1是髓樣分化蛋白2(MD2)的抑制劑,KD值為189 μM。
靶點(diǎn)
TargetValue
MD2
()
189 μM(Kd)
體外研究

Myeloid differentiation protein 2 (MD2) is a co-receptor of TLR4. Among those derivatives, MD2-IN-1 (compound 20) shows the strongest inhibitory effect on LPS-induced expression of both TNF-α and IL-6. Compare 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. 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.

體內(nèi)研究

Administration of MD2-IN-1 evidently reduces the LPS-induced increase in protein concentrations in BALF. The lung wet/dry weight ratio is markedly higher in the LPS-treated group than the control group, and MD2-IN-1 treatment reduces LPS-induced pulmonary edema. 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.

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