货号 | 15041-100mg |
描述 | Quinacrine, also commonly known as mepacrine, is a compound with multiple actions that is commonly used as an anti-protozoal agent.1 It potently prevents misfolding of prion protein (EC50 = 0.3 μM), blocks voltage-dependent sodium channels (IC50 = 3.3 μM), and inhibits aldehyde oxidase (IC50 = 3.3 μM).2,3,4 Quinacrine is also an effective riboflavin antagonist, associating with the riboflavin-binding protein (Ki = 6.7 μM), and inhibitor of P-glycoprotein (EC50 = 14.4 μM).5,6 At much higher doses, quinacrine inhibits phospholipase A2activity.7,8 |
别名 | Atebrine;Mepacrine; |
供应商 | Cayman |
应用文献 | |
1.Upcroft, P. and Upcroft, J.A. Drug targets and mechanisms of resistance in the anaerobic protozoa. Clin.Microbiol.Rev. 14(1), 150-164 (2001). 2.Vogtherr, M.,Grimme, S.,Elshorst, B., et al. Antimalarial drug quinacrine binds to C-terminal helix of cellular prion protein. Journal of Medicinal Chemistry 46(17), 3563-3564 (2003). 3.McNeal, E.T.,Lewandowski, G.A.,Daly, J.W., et al. [3H]Batrachotoxinin A 20α-benzoate binding to voltage-sensitive sodium channels: A rapid and quantitative assay for local anesthetic activity in a variety of drugs. Journal of Medicinal Chemistry 28(3), 381-388 (1985). 4.Pryde, D.C.,Dalvie, D.,Hu, Q., et al. Aldehyde oxidase: An enzyme of emerging importance in drug discovery. Journal of Medicinal Chemistry 53(24), 8441-8460 (2010). 5.Plantinga, A.,Witte, A.,Li, M.H., et al. Bioanalytical screening of riboflavin antagonists for targeted drug delivery - A thermodynamic and kinetic study. ACS Med.Chem.Lett. 2(5), 363-367 (2011). 6.Tiberghien, F. and Loor, F. Ranking of P-glycoprotein substates and inhibitors by a calcein-AM fluorometry screening assay. Anti-Cancer Drugs 7(5), 568-578 (1996). 7.Farooqui, A.A.,Ong, W.Y. and Horrocks, L.A. Inhibitors of brain phospholipase A2 activity: Their neuropharmacological effects and therapeutic importance for the treatment of neurologic disorders. Pharmacological Reviews 58(3), 591-620 (2006). 8.Caro, A.A. and Cederbaum, A.I. Role of phospholipase A2 activation and calcium in CYP2E1-dependent toxicity in HepG2 cells. The Journal of Biological Chemisty 278(36), 33866-33877 (2003). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 472.9 |
分子式 | C23H30ClN3O • 2HCl [XH2O] |
稳定性 | ≥ 2 years |
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