U-73122

U-73122 is an inhibitor of PLC-dependent processes, however, the mechanism of action remains unclear.1,2,3 The IC50 values for inhibition of platelet aggregation induced by collagen or thrombin are 0.6 and 5 µM, respectively.2 It also exhibits inhibitory activity against HIV-1 integrase with an IC50 value of 7 µM.4WARNING This product is not for human or veterinary use.

Inhibits PLC-dependent processes

464.6

≥95%

Biochemicals/Antivirals/Integrase Inhibitors

Formal_Name:1-[6-[[(17β)-3-methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrrole-2,5-dione

[H][C@@]12CCC3=CC(OC)=CC=C3[C@@]1([H])CC[C@@]4(C)[C@@]2([H])CC[C@@H]4N(CCCCCCN5C(C=CC5=O)=O)[H]

C29H40N2O3

112648-68-7

≥ 4 years

DMF: 3.3 mg/ml DMSO: 0.5 mg/ml Ethanol: <0.5 mg/ml (takes 24 h to diss

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).