CAS NO: | 2854-32-2 |
包装 | 价格(元) |
10mg | 电议 |
50mg | 电议 |
Storage | Store at -20°C |
M.Wt | 426.89 |
Cas No. | 2854-32-2 |
Formula | C23H23ClN2O4 |
Solubility | ≥42.7 mg/mL in DMSO with gentle warming; insoluble in EtOH; insoluble in H2O |
Chemical Name | 2-[1-(4-chlorobenzoyl)-5-methoxy-2-methylindol-3-yl]-1-morpholin-4-ylethanone |
Canonical SMILES | CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)N4CCOCC4 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
BML-190(IMMA)是有效的和选择性的CB2受体的配体(Ki值 = 435 nM).
大麻素受体(CB1和CB2)属于G蛋白偶联受体(GPCR),在各种生理过程中起着重要作用,如认知与免疫功能.
在表达人Cb2受体的HEK-293细胞中,BML-190促进毛喉素诱导的cAMP积累.此外,在表达CB2受体和16z44的细胞中,BML-190也减少磷酸肌醇的基础水平产生[1].
BML-190在LPS(脂多糖)激活的炎症中起着重要作用[2],能降低人细胞因子分泌并降低单核细胞神经毒性[3].BML-190促进成纤维细胞集落形成[4]并缓解胶原诱导的关节炎[5].
参考文献:
[1] New DC, Wong YH. BML-190 and AM251 act as inverse agonists at the human cannabinoid CB2 receptor: signalling via cAMP and inositol phosphates. FEBS Lett. 2003 Feb 11;536(1-3):157-60. PubMed PMID: 12586356.
[2] Chang YH, Lee ST, Lin WW. Effects of cannabinoids on LPS-stimulated inflammatory mediator release from macrophages: involvement of eicosanoids. J Cell Biochem. 2001;81(4):715-23. PubMed PMID: 11329626.
[3] Klegeris A, Bissonnette CJ, McGeer PL. Reduction of human monocytic cell neurotoxicity and cytokine secretion by ligands of the cannabinoid-type CB2 receptor. Br J Pharmacol. 2003 Jun;139(4):775-86. PubMed PMID: 12813001; PubMed Central PMCID: PMC1573900.
[4] Scutt A, Williamson EM. Cannabinoids stimulate fibroblastic colony formation by bone marrow cells indirectly via CB2 receptors. Calcif Tissue Int. 2007 Jan;80(1):50-9. Epub 2007 Jan 4. PubMed PMID: 17205329.
[5] Zhang L, Zhang X, Wu P, Li H, Jin S, Zhou X, Li Y, Ye D, Chen B, Wan J. BML-111, a lipoxin receptor agonist, modulates the immune response and reduces the severity of collagen-induced arthritis. Inflamm Res. 2008 Apr;57(4):157-62. doi: 10. 1007/s00011-007-7141-z. PubMed PMID: 18648754.
[6] Zhang Q, Ma P, Cole RB, Wang G. In vitro metabolism of indomethacin morpholinylamide (BML-190), an inverse agonist for the peripheral cannabinoid receptor (CB(2)) in rat liver microsomes. Eur J Pharm Sci. 2010 Sep 11;41(1):163-72. doi: 10.1016/j.ejps.2010.06.004. Epub 2010 Jun 11. PubMed PMID: 20542112; PubMed Central PMCID: PMC2907062.