U-73122是PLC依賴性過程的抑制劑，然而，其作用機(jī)制仍不清楚。[1]、[2]、[3]抑制膠原或凝血酶誘導(dǎo)的血小板聚集的IC50值分別為0.6和5M。它還表現(xiàn)出對(duì)HIV-1整合酶的抑制活性，IC50值為7M。[4]U-73343是U-73122的緊密結(jié)構(gòu)類似物，不抑制PLC，使其可用作PLC抑制的陰性對(duì)照。[1]

產(chǎn)品性質(zhì)：

Cas No.:142878-12-4

化學(xué)名: 1-(6-(((8R,9S,13S,14S,17S)-3-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-17-yl)amino)hexyl)pyrrolidine-2,5-dione

Canonical SMILES: C[C@]12CC[C@]3([H])C4=CC=C(OC)C=C4CC[C@@]3([H])[C@]1([H])CC[C@]2([H])NCCCCCCN5C(CCC5=O)=O

分子式:C29H42N2O3

分子量:466.66

溶解度:0.25mg/ml in ethanol; 0.5mg/ml in DMSO; 2mg/ml in DMF

儲(chǔ)存條件:Store at -20°C

注意事項(xiàng)：

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References:

[1]. Smith, R.J., Sam, L.M., Justen, J.M., et al. Receptor-coupled signal transduction in human polymorphonuclear neutrophils: Effects of a novel inhibitor of phospholipase C-dependent processes on cell responsiveness. Journal of Pharmacology and Experimental Therapeutics 253, 688-697 (1990).

[2]. Bleasdale, J.E., Thakur, N.R., Gremban, R.S., et al. Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils. Journal of Pharmacology and Experimental Therapeutics 255, 756-768 (1990).

[3]. Hildebrandt, J.P., Plant, T.D., and Meves, H. The effects of bradykinin on K+ currents in NG108-15 cells treated with U73122, a phospholipase C inhibitor, or neomycin. British Journal of Pharmacology 120, 841-850 (1997).

[4]. Burke, T.R., Jr., Fesen, M.R., Mazumder, A., et al. Hydroxylated aromatic inhibitors of HIV-1 integrase. Journal of Medicinal Chemistry 38, 4171-4178 (1995).