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U73122

Cat. No. M5170

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U73122 Structure
Synonym:

U-73122

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5mg USD 64 In stock
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Biological Activity

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.

Chemical Information
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
References

[1] Klein RR, et al. J Biol Chem. Direct activation of human phospholipase C by its well known inhibitor u73122.

[2] Smith RJ, et al. J Pharmacol Exp Ther. Receptor-coupled signal transduction in human polymorphonuclear neutrophils: effects of a novel inhibitor of phospholipase C-dependent processes on cell responsiveness.

[3] Bleasdale JE, et al. J Pharmacol Exp Ther. Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils.

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Keywords: U73122, U-73122 supplier, Phospholipase, inhibitors, activators

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