中文名 | MDL-29951 |
英文名 | 2-Carboxy-4,6-dichloro-1H-indole-3-propionic acid |
别名 | 2-羧基-4,6-二氯-1H-吲哚-3-丙酸 |
英文别名 | CS-1105 MDL29951 MDL-29951 2-Carboxy-4,6-dichloro-1H-indole-3-propionic acid 2-Carboxy-4,6-dichloro-1H-indole-3-propanoic acid 3-(2-carboxy-4,6-dichloroindol-3-yl)propionic acid 3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid MDL-29951 2-Carboxy-4,6-dichloro-1H-indole-3-propanoic acid |
CAS | 130798-51-5 |
EINECS | 200-256-5 |
化学式 | C12H9Cl2NO4 |
分子量 | 302.11 |
密度 | 1.657±0.06 g/cm3(Predicted) |
熔点 | 273-280℃ |
沸点 | 582.5±45.0 °C(Predicted) |
溶解度 | 溶于DMSO (升温至15 mg/ml) 或乙醇 (高达10 mg/ml)。 |
酸度系数 | 4.04±0.30(Predicted) |
存储条件 | 2-8°C(protect from light) |
稳定性 | 自pruchase提供之日起稳定2年。在DMSO或乙醇中的溶液可以在-20 ° 储存长达3个月。 |
外观 | 固体 |
颜色 | Off-white |
体外研究 | 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. |
上游原料 | 2-氧代环戊羧酸乙酯 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.31 ml | 16.55 ml | 33.101 ml |
5 mM | 0.662 ml | 3.31 ml | 6.62 ml |
10 mM | 0.331 ml | 1.655 ml | 3.31 ml |
5 mM | 0.066 ml | 0.331 ml | 0.662 ml |
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