吲哚美辛吗啉代酰胺 T6417

Product Introduction
Bioactivity


英文名: BML-190

描述: BML-190 (Indomethacin morpholinylamide) 是一种 CB2 受体的配体，其对 CB2 受体 (Ki:435 nM) 和 CB1受体 (Ki> 2 μM)。

细胞实验: 293/CB2 cells are labeled with [3H]adenine (1 μCi/mL) in MEM with 1% FBS for 20 hours-24 hours. Labelled cells are challenged with 50 μM forskolin and appropriate BML-190 for 30 minutes at 37°C and assayed for cAMP accumulation. For IP assays, 2 × 105 293/CB2 cells are transiently transfected with 16z44 and/or pcDNA3 using transfection reagents. Cells are labelled, challenged with BML-190 and assayed for IP production. Triplicates are performed for each data point and at least three separate trials are done for each ligand.(Only for Reference)

体外活性: BML-190 has 50-fold selectivity for CB2 receptors over CB1 receptors. In HEK-293 cells stably expressing the human CB2 receptor, BML-190 potentiates the forskolin-stimulated accumulation of cAMP. BML-190 reduces the basal levels of inositol phosphate production in cells expressing the CB2 receptor. 10 μM of BML-190 decreases inositol phosphates accumulation by 38%. [1] BML-190 is an aminoalkylindole. BML-190 is found to yield at least 15 metabolic products. [2] BML-190 diminishes LPS-induced NO and IL-6 production in a concentration-dependent manner. BML-190 also inhibits LPS-induced PGE2 production and COX-2 induction. [3]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 21 mg/mL (49.2 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: inhibit | Cannabinoid Receptor | Inhibitor | BML190 | BML-190

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相关库: Anti-Neurodegenerative Disease Compound Library | Bioactive Lipid Compound Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | GPCR Compound Library | Anti-Fibrosis Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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