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MDL 29951  ≥98%(HPLC)

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包装规格：5mg 25mg 100mg in glass bottle
溶解性：溶于DMSO(≥50mg/mL)
产品描述：基本信息 产品编号： M10316 产品名称： MDL 29951 CAS: 130798-51-5   储存条件 粉末 -20℃ 四年     分子式： C12H9Cl2NO4 溶于液体 -80℃ 6个月 分子量： 302.11 -20℃ 1个月 化学名：  2-Carboxy-4,6-dichloro-1H-indole-3-propanoic acid Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 3.3101mL 16.5503mL 33.1005mL 5mM 0.6620mL 3.3101mL 6.6201mL 10mM 0.3310mL 1.6550mL 3.3101mL   生物活性 产品描述 一种nMDA receptor拮抗剂，可抑制体内体外甘氨酸([3H]glycine)的结合，Ki值为0.14μM。 靶点 Ki:0.14μM   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 (IC50=2.5μM).MDL-29951 inhibits the human liver (IC50=2.5μM),porcine kidney (IC50=1.0μM),and rabbit liver (IC50=0.21μM) isoforms of the enzyme,but is significantly less potent against the rat liver isoform (IC50=11μM).The MDL29951-activated receptor exhibits other activities associated with GPCR-mediated signaling, including G protein-dependent activation of extracellular signalregulated 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.     推荐实验方法(仅供参考) 激酶实验： [3H]JCPP (30.7 Ci/mmol) binding assays are conducted in minivials,incubated for 15mm at 25℃ in 1mL of 50mM Tris-HC1 (pH 7.4) containing 10nM [3H]JCPP,200g of membrane protein and unlabeled ligands as indicated.Nonspecific binding is defined using 1mM L-glutamate.Bound ligand is separated by centrifugation. Specific binding accounted for approximately 80% of total binding.
保存条件：-20℃

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