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 |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
| Related Phospholipase Products |
|---|
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Phospholipase A2 (PLA2) catalyzes the hydrolysis of the sn-2 position of membrane glycerophospholipids to liberate arachidonic acid (AA). |
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Melittin is a PLA2 activator that stimulates the activity of low molecular weight PLA2 without increasing the activity of high molecular weight PLA2. |
| trans-4-phenylbut-3-en-2-one
trans-Benzylideneacetone (trans-Benzalacetone), a metabolite of gram-negative entomopathogenic bacterium Xenorhabdus nematophila, is an enzyme inhibitor against phospholipase A2 (PLA2). |
| SYN-020
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| IIAEK
IIAEK is a novel cholesterol-lowering pentapeptide derived from bovine milk β-lactoglobulin that targets intestinal alkaline phosphatase (IAP) and improves cholesterol metabolism through the specific activation of IAP and down-regulation of ABCA1. Sequence: Ile-Ile-Ala-Glu-Lys |
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