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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)。
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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)。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
2 mg | ¥ 108 | 现货 | |
5 mg | ¥ 153 | 现货 | |
10 mg | ¥ 259 | 现货 | |
25 mg | ¥ 496 | 现货 | |
50 mg | ¥ 818 | 现货 | |
100 mg | ¥ 1,350 | 现货 | |
200 mg | ¥ 2,320 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 167 | 现货 |
产品描述 | BML-190 (Indomethacin morpholinylamide) is a specific CB2 receptor inverse agonist (Ki: 435 nM), with 50-fold selectivity over CB1 receptor. |
靶点活性 | CB2:435 nM(Ki) |
体外活性 | BML-190 在针对CB2受体相比CB1受体展现出50倍的选择性。在稳定表达人类CB2受体的HEK-293细胞中,BML-190增强了forskolin刺激下的cAMP积累。同时,BML-190降低了表达CB2受体细胞中肌醇磷酸基本水平,10 μM BML-190使肌醇磷酸积累减少38%。[1] BML-190是一种氨基烷基吲哚,已发现能产生至少15种代谢产物。[2] 在浓度依赖性的方式中,BML-190减少了LPS诱导的NO及IL-6产生,并且抑制了LPS诱导的PGE2产生与COX-2的诱导。[3] |
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) |
别名 | 吲哚美辛吗啉代酰胺, Indomethacin morpholinylamide, IMMA, BML 190, 2-[1-(4-氯苯甲酰基)-5-甲氧基-2-甲基-1H-吲哚-3-基]-1-(4-吗啉基)乙酮 |
分子量 | 426.89 |
分子式 | C23H23ClN2O4 |
CAS No. | 2854-32-2 |
Smiles | COc1ccc2n(C(=O)c3ccc(Cl)cc3)c(C)c(CC(=O)N3CCOCC3)c2c1 |
密度 | 1.31 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | DMSO: 21 mg/mL (49.2 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||
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