U73122 is a potent inhibitor of phospholipase C, phospholipase A2 and 5-LO (5-lipoxygenase), which reduces agonist-induced Ca2+ increases in platelets and PMN. U-73122 inhibits agonist-induced phospholipase C (IC50=1.0-2.1 μM) activation in neutrophils and human platelets. 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 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. U73122 (30 mg/kg i.p.) blocks swelling of rats hind paw by 65 and 80% at 1 and 3 h postcarrageenan challenge. 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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMF 24 mg/mL warming|
Direct activation of human phospholipase C by its well known inhibitor u73122.
Klein RR, et al. J Biol Chem. 2011 Apr 8;286(14):12407-16. PMID: 21266572.
Receptor-coupled signal transduction in human polymorphonuclear neutrophils: effects of a novel inhibitor of phospholipase C-dependent processes on cell responsiveness.
Smith RJ, et al. J Pharmacol Exp Ther. 1990 May;253(2):688-97. PMID: 2338654.
Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils.
Bleasdale JE, et al. J Pharmacol Exp Ther. 1990 Nov;255(2):756-68. PMID: 2147038.
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