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U73122

Cat. No. M5170

U73122 Structure

Synonym: U-73122

Size Price Availability Quantity
5mg USD 80 In stock
10mg USD 120 In stock
50mg USD 420 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 464.64
Formula C29H40N2O3
CAS Number 112648-68-7
Purity >99%
Solubility DMF 24 mg/mL warming
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




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

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