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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.
| Molecular Weight | 464.64 |
| Formula | C29H40N2O3 |
| CAS Number | 112648-68-7 |
| Solubility (25°C) | DMF 20 mg/mL warming |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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