Inhibits PLC-dependent processes
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U-73122

Item No. 70740

Technical Information
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
Purity
≥95%
A crystalline solid
DMF: 3.3 mg/mlDMSO: 0.5 mg/mlEthanol: <0.5 mg/ml (takes 24 h to diss
SMILES
[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]
InChi Code
InChI=1S/C29H40N2O3/c1-29-16-15-23-22-10-8-21(34-2)19-20(22)7-9-24(23)25(29)11-12-26(29)30-17-5-3-4-6-18-31-27(32)13-14-28(31)33/h8,10,13-14,19,23-26,30H,3-7,9,11-12,15-18H2,1-2H3/t23-,24-,25+,26+,29+/m1/s1
InChi Key
LUFAORPFSVMJIW-ZRJUGLEFSA-N
Shipping & Storage Information
Storage
Room temperature
Shipping
Room temperature in continental US; may vary elsewhere
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    Product 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 are 0.6 and 5 µM, respectively.2 It also exhibits inhibitory activity against HIV-1 integrase with an IC50 value of 7 µM.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Smith, R.J., Sam, L.M., Justen, J.M., et alReceptor-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(2), 688-697 (1990).

    2. Bleasdale, J.E., Thakur, N.R., Gremban, R.S., et alSelective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils. J. Pharmacol. Exp. Ther. 255(2), 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. Br. J. Pharmacol. 120(5), 841-850 (1997).

    4. Burke, T.R., Jr., Fesen, M.R., Mazumder, A., et alHydroxylated aromatic inhibitors of HIV-1 integrase. J. Med. Chem. 38(21), 4171-4178 (1995).