MDL-29951
| 中文名稱 | MDL-29951 |
|---|---|
| 中文同義詞 | 2-羧基-4,6-二氯-1H-吲哚-3-丙酸;化合物MDL 29951,10 MM DMSO 溶液 |
| 英文名稱 | MDL-29951 |
| 英文同義詞 | 2-Carboxy-4,6-dichloro-1H-indole-3-propionic acid;3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid;2-Carboxy-4,6-dichloro-1H-indole-3-propanoic acid;MDL-29951 2-Carboxy-4,6-dichloro-1H-indole-3-propanoic acid;MDL-29951, >=98%;3-(2-carboxy-4,6-dichloroindol-3-yl)propionic acid;CS-1105;MDL-29951; MDL29951 |
| CAS號 | 130798-51-5 |
| 分子式 | C12H9Cl2NO4 |
| 分子量 | 302.11 |
| EINECS號 | 200-256-5 |
| 相關(guān)類別 | 小分子抑制劑;小分子抑制劑，天然產(chǎn)物;Inhibitors |
| Mol文件 | 130798-51-5.mol |
| 結(jié)構(gòu)式 |  |
MDL-29951 性質(zhì)
| 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 | 2-8°C(protect from light) |
| 溶解度 | 可溶于DMSO（加熱時高達15mg/ml）或乙醇（高達10mg/ml）。 |
| 形態(tài) | 固體 |
| 酸度系數(shù)(pKa) | 4.04±0.30(Predicted) |
| 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。 |
Ki: 0.14 μM
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.