U-73122 is a potent phospholipase C (PLC) inhibitor with IC50 value of ~6 μM [1].
PLC is a class of membrane-associated enzymes that catalyzes the hydrolysis of a membrane phospholipid, phosphatidylinositol 4,5-bisphosphate (PIP2), to produce two intracellular messengers, diacylglycerol and inositol-triphosphate, which, in turn, mediate the activation of protein kinase C (PKC) and intracellular Ca2+ release, respectively. It plays an important role in various signal transduction pathways [1].
U-73122 significantly inhibited recombinant human PLC-β2 with IC50 value of ~6 μM, while showing little effect on PLC-β1, PLC-β3 or PLC-β4. In human neutrophils, U-73122 reduced interleukin-8 and leukotriene B4-induced Ca2+ flux and chemotaxis with IC50 values of ~6 μM and ~5 μM, respectively [1].
In rats, U-73122 (30 mg/kg, i.p.) inhibited hind paw swelling by 65% and 80% at 1 h and 3 h post-carrageenan challenge. Moreover, pretreatment of U-73122 (1 mg/kg, 3 mg/kg and 10 mg/kg, respectively, i.v.) effectively suppressed TPA-induced mouse ear edema in a dose-dependent manner [1].
Reference:
[1]. Hou C, Kirchner T, Singer M, et al. In vivo activity of a phospholipase C inhibitor, 1-(6-((17beta-3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione (U73122), in acute and chronic inflammatory reactions. Journal of Pharmacology and Experimental Therapeutics, 2004, 309(2): 697-704.
Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
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We do not recommend long-term storage for the solution, please use it up soon.
Protocol
Cell experiment:[1]
Cell lines
Human neutrophils
Reaction Conditions
15 min or 3 h incubation
Applications
In human neutrophils, U-73122 reduced interleukin-8 and leukotriene B4-induced Ca2+ flux (after 15 min incubation) and chemotaxis (after 3 h incubation) in a concentration-dependent manner, with IC50 values being ~6 μM and ~5 μM, respectively.
Animal experiment:[1]
Animal models
Male Sprague-Dawley rats, ~ 200 g
Dosage form
30 mg/kg
Administered intraperitoneally (i.p.)
Applications
In rats, U-73122 (30 mg/kg, i.p.) inhibited hind paw swelling by 65% and 80% at 1 h and 3 h post-carrageenan challenge. U-73122 significantly inhibited carrageenan-induced inflammation, and its effect was more complete than a 10 mg/kg p.o. dose of indomethacin.
Note
The technical data provided above is for reference only.
References:
1. Hou C, Kirchner T, Singer M, et al. In vivo activity of a phospholipase C inhibitor, 1-(6-((17beta-3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione (U73122), in acute and chronic inflammatory reactions. Journal of Pharmacology and Experimental Therapeutics, 2004, 309(2): 697-704.
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