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    U73122
    U73122

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0845
    CAS #: 112648-68-7Purity ≥98%

    Description: U73122 (U 73122; U-73122) is a novel and potent phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with potential anti-inflammatory activity. It inhibits PLC with an IC50 of 1-2.1 µM. U73122 can also acts as an inhibitor of myocardial PLD by interaction with PIP2 as a cofactor for optimal PLD activity.

    References: J Pharmacol Exp Ther. 1990 Nov;255(2):756-68; J Pharmacol Exp Ther. 2004 May;309(2):697-704. 

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    Molecular Weight (MW)464.64
    FormulaC29H40N2O3
    CAS No.112648-68-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 0.01 mg/mL warmed (0.02 mM)
    Water: <1 mg/mL
    Ethanol:N/A
    Solubility (In vivo)2% Tween 80+saline: 5mg/mL 
    SynonymsU 73122; U73122; U73122. 

    Chemical Name: 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)-1H-pyrrole-2,5-dione

    InChi Key: LUFAORPFSVMJIW-ZRJUGLEFSA-N

    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

    SMILES Code: O=C(C=C1)N(CCCCCCN[[email protected]]2CC[[email protected]@]3([H])[[email protected]]4([H])CCC5=CC(OC)=CC=C5[[email protected]@]4([H])CC[[email protected]]23C)C1=O           


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    In Vitro

    In vitro activity:  U73122 significantly inhibits aggregation of human platelets induced by a variety of agonists, including collagen, thrombin, ADP, arachidonic acid, with IC50 of 1-5 μM. U-73122 (10 μM) inhibits the production of IP3 and the subsequent rapid increase in cytosolic Ca2+ induced by either thrombin or U-46619 through inhibiting hydrolysis of phosphatidyl[3H]inositol and phosphatldyl[3H]inosito1 4,5-bisphosphate catalyzed by a soluble fraction from platelets (Ki=9 and 40 μM, respectively). U-73122 inhibits thromboxane B production induced by collagen through inhibiting receptor-coupled mobilization of arachidonic acid. U73122 inhibits also FMLP-induced aggregation of human polymorphonuclear neutrophils and the associated production of IP3 and diacylglycerol. U-73122 causes a concentration-dependent inhibition of C5a, FMLP, PAF and LTB4-induced MPO and B12-BP release from cyto-chalasin B-treated PMNs. The IC50 values are 60 (FMLP), 110 (LTB4), 115 (C5a) and 120 (PAF) nM for MPO release; and 105 (FMLP), 110 (LTB4), 120 (C5a) and 140 (PAY) nM for B12-BP release. U-73122 is also a potent inhibitor of superoxide anion production by cytochalasin B-treated PMNs activated with either C5a or FMLP with IC50 of 160 and 300 nM, respectively. U-73122 causes suppression of the rise in [Ca2+]i, IP3 production and DAG production in FMLP-stimulated PMNs with IC50 of 500 nM, 2 μM, and 2 μM, respectively. 3 μM U-73122 causes 100% inhibition of FMLP-induced GTPase activity. U-73122 causes a concentration-dependent inhibition of the FMLP-evoked association of PKC with the extractable particulate fraction of PMNs, but not a soluble preparation of PMN PKC. U73122 significantly inhibits recombinant human PLC-β2, with an IC50 of ~6 μM. U73122 has little effect on PLC-β1, PLC-β3, or PLC-β4. U73122 reduces interleukin-8 and leukotriene B4-induced Ca2+ flux and chemotaxis in human neutrophils with IC50 of ~6 μM and ~5 μM, respectively.


    Kinase Assay: U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50 of 1-2.1 µM for PLC.


    Cell Assay: Agonist-induced production of IP3 in PMN is measured by use of the competitive radiobinding assy. PMN (2 x 106-107) in 0.2 mL of phosphate-buffered saline, pH 7.4 [NaC1 (138 mM), Na2HPO4 (8.1 mM), KH2PO4 (1.5 mM), KCI (2.7 mM), CaCl2 (1.0 mM), MgC12 (1.0 mM) and glucose (0.1%, w/v)] are incubated in conical polypropylene tubes at 37°C in a shaking water bath. U-73122 or U-73343 is added (in 1 μL of DMSO) 3 min before the addition of agonist, FMLP (0.1 μM) plus cytochalasin B (5 μg/mL). FMLP and cytochalasin B are added in 1 μL each of DMSO and ethanol, respectively. Appropriate vehicle controls are included in each experiment. PMN incubation mixtures are quenched with the addition of 0.07 mL of ice-cold TCA (20%, w/v) and a portion (0.2 mL) of the TCA extract is processed for the measurement of IP3 by competitive radiobinding as described above for platelets.

    In VivoU73122 (30 mg/kg i.p.) blocks swelling of rats hind paw by 65 and 80% at 1 and 3 h postcarrageenan challenge. U73122 (0.1 mg/mL) inhibits carrageenan-induced macrophage and lymphocyte accumulation into subcutaneous chambers in dogs by 65 and 74%, respectively. U73122 (30 mg/kg i.p.) totally inhibits the LPS-induced increase in macrophage and lymphocyte infiltration and prostaglandin E2 production (by 80%) in a mouse peritonitis model, and inhibits and 12- O-tetradecanoyl-phorbol-13-acetate-induced ear edema in mice.
    Animal modelRats
    Formulation & Dosage30 mg/kg i.p.
    ReferencesJ Pharmacol Exp Ther. 1990 Nov;255(2):756-68; J Pharmacol Exp Ther. 2004 May;309(2):697-704. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    U73122

    Effects of U73122 and its analog U73343 on the hydrolysis of [3H]PIP2 by PLC-β isozymes.



    U73122

    Effect of U73122 on TPA-induced ear edema in mice. J Pharmacol Exp Ther. 2004 May;309(2):697-704.
     

    U73122

    Effect of U73122 on IL-8- and LTB4-induced Ca2+ mobilization in human neutrophils. J Pharmacol Exp Ther. 2004 May;309(2):697-704.
     

    U73122

    Anti-inflammatory effects of U73122 and indomethacin on carrageenan-induced hind paw edema in rats.


    U73122

    U73122 inhibits LPS-induced PGE2 production in peritoneal lavage fluid. J Pharmacol Exp Ther.2004 May;309(2):697-704.


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