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U-73122

Cayman Chemical Item Number 70740

(CAS 112648-68-7)

U-73122 (CAS 112648-68-7)

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Description

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 is 0.6 and 5 µM, respectively.2 It also exhibits inhibitory activity against HIV-1 integrase with an IC50 value of 7 µM.4

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. J Pharmacol Exp Ther 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. J Pharmacol Exp Ther 255 756-768 (1990).

3 Hildebrandt, J., 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. Br J Pharmacol 120 841-850 (1997).

4 Burke, T.R., Fesen, M.R., Mazumder, A., et al. Hydroxylated aromatic inhibitors of HIV-1 integrase. J Med Chem 38 4171-4178 (1995).

Formal Name 1-​[6-​[[(17β)-​3-​methoxyestra-​1,​3,​5(10)-​trien-​17-​yl]amino]hexyl]-​1H-​pyrrole-​2,​5-​dione
CAS Number 112648-68-7
Molecular Formula C29H40N2O3
Formula Weight 464.6
Formulation A crystalline solid
Purity ≥97%
Stability 1 year
Storage Room temperature
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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[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]​

Background Reading

Thompson, A.K., Mostafapour, S.P., Denlinger, L.C., et al. The aminosteroid U-73122 inhibits muscarinic receptor sequestration and phosphoinositide hydrolysis in SK-N-SH neuroblastoma cells. A role for Gp in receptor compartmentation. J Biol Chem 266 23856-23862 (1991).

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. J Pharmacol Exp Ther 255 756-768 (1990).

Burke, T.R., Fesen, M.R., Mazumder, A., et al. Hydroxylated aromatic inhibitors of HIV-1 integrase. J Med Chem 38 4171-4178 (1995).

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. J Pharmacol Exp Ther 253 688-697 (1990).

Hildebrandt, J., 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. Br J Pharmacol 120 841-850 (1997).

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