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MDL-29951
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产品介绍
产品介绍
产品信息
抗原名称
NMDA:0.14 μM
简单描述
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=0.14 μM。
商品描述
MDL-29951 is a novel glycine antagonist of NMDA receptor activation.
分子量
302.11
纯度
99.49%
性状
0
颜色
0
In vitro(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[1]. MDL-29951 is found to inhibit the human F16Bpase under these conditions (IC50=2.5 μM). MDL-29951 inhibits the human liver (IC50=2.5 μM), porcine kidney (IC50=1.0 μM), and rabbit liver (IC50=0.21 μM) isoforms of the enzyme, but is significantly less potent against the rat liver isoform (IC50=11 μM)[2]. 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 Ca2+ 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[3].
In vivo(体内研究)
0
背景
别名
0
分子式
C12H9Cl2NO4
CAS号
130798-51-5
密度
1.657 g/cm3 (Predicted)
制备和贮存
溶解方法
DMSO: 50 mg/mL (165.5 mM), Sonication is recommended.
存储溶液
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
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