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MDL-29951
产品纠错
CAS号:130798-51-5 | 英文名称:MDL-29951
分子式 C12H9Cl2NO4
分子量 302
EINECS号 200-256-5
MDL MFCD00897722
Smiles
InChIKey
乙二醇化学百科
基本信息
中文名称 MDL-29951
英文名称 MDL-29951
CAS号 130798-51-5
分子式 C12H9Cl2NO4
分子量 302.11
EINECS号 200-256-5
物化性质
熔点 273-280℃
沸点 582.5±45.0 °C(Predicted)
密度 1.657±0.06 g/cm3(Predicted)
溶解度 可溶于DMSO(加热时高达15mg/ml)或乙醇(高达10mg/ml)。
形态 固体
酸度系数(pKa) 4.04±0.30(Predicted)
颜色 米白色
稳定性 DMSO或乙醇溶液可在-20°下稳定储存3个月。
安全信息
生产及用途
MDL-29951 是一种新颖的 nMDA receptor 拮抗剂,能够抑制体内体外甘氨酸 ([3H]glycine) 的结合,Ki 值为 0.14 μM。

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.

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