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130798-51-5

中文名稱 MDL-29951
英文名稱 MDL-29951
CAS 130798-51-5
分子式 C12H9Cl2NO4
分子量 302.11
MOL 文件 130798-51-5.mol
更新日期 2024/12/10 12:36:18
130798-51-5 結構式 130798-51-5 結構式

基本信息

中文別名
2-羧基-4,6-二氯-1H-吲哚-3-丙酸
英文別名
CS-1105
MDL-29951, >=98%
MDL-29951
MDL29951
2-Carboxy-4,6-dichloro-1H-indole-3-propanoic acid
2-Carboxy-4,6-dichloro-1H-indole-3-propionic acid
3-(2-carboxy-4,6-dichloroindol-3-yl)propionic acid
1H-Indole-3-propanoic acid, 2-carboxy-4,6-dichloro-
3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid
MDL-29951 2-Carboxy-4,6-dichloro-1H-indole-3-propanoic acid

物理化學性質

熔點273-280℃
沸點582.5±45.0 °C(Predicted)
密度1.657±0.06 g/cm3(Predicted)
儲存條件Keep in dark place,Sealed in dry,2-8°C
溶解度可溶于DMSO(加熱時高達15mg/ml)或乙醇(高達10mg/ml)。
酸度系數(pKa)4.04±0.30(Predicted)
形態(tài)固體
顏色米白色
穩(wěn)定性DMSO或乙醇溶液可在-20°下穩(wěn)定儲存3個月。

安全數據

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H317

常見問題列表

生物活性
MDL-29951 是一種新穎的 nMDA receptor 拮抗劑,能夠抑制體內體外甘氨酸 ([3H]glycine) 的結合,Ki 值為 0.14 μM。
靶點

Ki: 0.14 μM

體外研究

MDL 100,748 and MDL 29,951 are approximately 2000-fold selective for the glycine binding site relative to the glutamate recognition sites. MDL-29951 is found to inhibit the human F16Bpase under these conditions (IC 50 =2.5 μM). MDL-29951 inhibits the human liver (IC 50 =2.5 μM), porcine kidney (IC 50 =1.0 μM), and rabbit liver (IC 50 =0.21 μM) isoforms of the enzyme, but is significantly less potent against the rat liver isoform (IC 50 =11 μM). The MDL29951-activated receptor exhibits other activities associated with GPCR-mediated signaling, including G protein-dependent activation of extracellular signal-regulated kinase 1 and 2 (ERK1/2) and recruitment of β-arrestin. As with recombinant cell systems, MDL29951 promotes Ca 2+ signaling responses and inhibition of cyclic adenosine monophosphate (cAMP) accumulation in rat oligodendrocyte precursor cells during the period of peak GPR17 abundance. Effects of MDL29951 are markedly reduced in cells with low GPR17 abundance and are blocked by pranlukast.

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