| 中文名称 |
BML-190
|
| 中文别名 |
2-(1-(4-氯苯甲酰基)-5-甲氧基-2-甲基-1H-吲哚-3-基)-1-吗啉乙酮;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
|
| 英文名称 |
BML-190
|
| 英文别名 |
2-(1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)-1-morpholinoethanone;BML-190;2-[1-(4-chlorobenzoyl)-5-methoxy-2-methylindol-3-yl]-1-morpholin-4-ylethanone;BML 190;Ethanone,2-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]-1-(4-morpholinyl)-;IMMA;2-Methyl-5-methoxy-3-indolyl-essigsaeure-amid;Ethanone (2-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]-1-(4-morpholinyl);Indomethacin morpholinamide;Indomethacin Morpholinylamide;Lopac-I-151;Tocris-1383;2-[1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]-1-(4-morpholinyl)ethanone;1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-3-[2-(4-morpholinyl)-2-oxoethyl]-1H-indole;1-(p-chlorobenzoyl)-5-methoxy-2-methyl-3-[(morpholinocarbonyl)methyl]-indole
|
| Cas No. |
2854-32-2
|
| 分子式 |
C23H23N2O4Cl
|
| 分子量 |
426.89
|
| 包装储存 |
Powder -20°C 3 years;4°C 2 years
|
| 详情描述 |
BML-190(IMMA)是CB2受体的配体,对CB2和CB1受体的Ki分别为435 nM和> 2 μM。
|
| 产品详情 |
BML-190(IMMA)是CB2受体的配体,对CB2和CB1受体的Ki分别为435 nM和> 2 μM。
|
| 生物活性 |
BML-190(IMMA) is a potent and selective CB2 receptor ligand (Ki values are 435 nM and > 2 μM for CB2 and CB1 respectively).
IC50 Value: 435 nM(Ki CB2)
Target:CB2 receptor
in vitro: BML-190 increases the accumulation of cAMP, via forskolin-stimulated mechanism in HEK-293 cells. Alternate studies suggest that BML-190 reduces the toxicity of culture supernatants to SH-SY5Y human neutroblastoma cells. Various research suggests that BML-190 is an essential tool in studying the proliferation of neuroblastoma. 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.
in vivo:
|
| 性状 |
Solid
|
| 运输条件 |
Room temperature in continental US; may vary elsewhere.
|
| 储存方式 |
Powder -20°C 3 years;4°C 2 years
|
| 参考文献 |
[1]. Zhang, Qiang; Ma, Peng; Cole, Richard B.; Wang, Guangdi In vitro metabolism of indomethacin morpholinylamide (BML-190), an inverse agonist for the peripheral cannabinoid receptor (CB2) in rat liver microsomes. European Journal of Pharmaceutical Sciences ([2]. Klegeris, Andis; Bissonnette, Christopher J.; McGeer, Patrick L. Reduction of human monocytic cell neurotoxicity and cytokine secretion by ligands of the cannabinoid-type CB2 receptor. British Journal of Pharmacology (2003), 139(4), 775-786.
|
| 溶解度数据 |
In Vitro: DMSO : 50 mg/mL (117.13 mM; Need ultrasonic)配制储备液
|
[1]. Zhang, Qiang; Ma, Peng; Cole, Richard B.; Wang, Guangdi In vitro metabolism of indomethacin morpholinylamide (BML-190), an inverse agonist for the peripheral cannabinoid receptor (CB2) in rat liver microsomes. European Journal of Pharmaceutical Sciences ([2]. Klegeris, Andis; Bissonnette, Christopher J.; McGeer, Patrick L. Reduction of human monocytic cell neurotoxicity and cytokine secretion by ligands of the cannabinoid-type CB2 receptor. British Journal of Pharmacology (2003), 139(4), 775-786.
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。