U73122

Alias: U 73122; U73122; U73122.
Cat No.:V0845 Purity: ≥98%
U73122 (U 73122; U-73122) is a novel and potent phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with potential anti-inflammatory activity.
U73122 Chemical Structure CAS No.: 112648-68-7
Product category: Phospholipase
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

U73122 (U 73122; U-73122) is a novel and potent phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with potential anti-inflammatory activity. It inhibits PLC with an IC50 of 1-2.1 µM. U73122 can also acts as an inhibitor of myocardial PLD by interaction with PIP2 as a cofactor for optimal PLD activity.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
In membranes separated from PMNs, U-73122 efficiently suppresses receptor-coupled activation of PLC [1]. Human polymorphonuclear neutrophil (PMN) aggregation induced by N-formyl-methionyl-leucyl-phenylalanine and the corresponding synthesis of diacylglycerol and IP3 are inhibited by U-73122 [2]. In digitonin-permeabilized cells, U-73122 dramatically inhibits phosphoinositide release caused by oxotremorine-M or guanosine-5'-O- (3-thiotriphosphate), but not by the addition of Ca2+ [3].
ln Vivo
In endotoxemic mice, U73122 markedly enhanced cardiac work, contraction and relaxation rates, without changing heart rate, while it had no effect on sham animals and greatly decreased TNF-α mRNA expression [4]. When compared to vehicle infusion into the VTA, U73122 (400 nM/μL) significantly decreased the overall length of lordosis in hamsters that were induced with estrogen and progesterone. The locomotor behavior of the hamsters in the activity monitor was not affected by the VTA infusion of U73122; however, muscimol significantly decreased the overall number of beam interruptions when compared to hamsters given SKF38393 [5].
Animal Protocol
30 mg/kg i.p.
Rats
References
[1]. Smith RJ, et al. Receptor-coupled signal transduction in human polymorphonuclear neutrophils: effects of a novel inhibitor of phospholipase C-dependent processes on cell responsiveness. J Pharmacol Exp Ther. 1990 May;253(2):688-97.
[2]. Bleasdale JE, et al. Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils. J Pharmacol Exp Ther. 1990 Nov;255(2):756-68.
[3]. Thompson AK, et al. The aminosteroid U-73122 inhibits muscarinic receptor sequestration and phosphoinositide hydrolysis in SK-N-SH neuroblastoma cells. A role for Gp in receptor compartmentation. J Biol Chem. 1991 Dec 15;266(35):23856-62.
[4]. Peng T, et al. Disruption of phospholipase Cgamma1 signalling attenuates cardiac tumor necrosis factor-alpha expression and improves myocardial function during endotoxemia. Cardiovasc Res. 2008 Apr 1;78(1):90-7. Epub 2007 Dec 12.
[5]. Frye CA, et al. In the ventral tegmental area, the membrane-mediated actions of progestins for lordosis of hormone-primed hamsters involve phospholipase C and protein kinase C. J Neuroendocrinol. 2007 Sep;19(9):717-24.
[6]. Hörnig M, et al. Inhibition of 5-lipoxygenase by U73122 is due to covalent binding to cysteine 416. Biochim Biophys Acta. 2012 Feb;1821(2):279-86.
[7]. Xie W, et al. 3Beta-hydroxy-6-aza-cholestane and related analogues as phosphatidylinositol specific phospholipase C (PI-PLC) inhibitors with antitumor activity. Bioorg Med Chem. 2000 Apr;8(4):699-70
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C29H40N2O3
Molecular Weight
464.64
CAS #
112648-68-7
SMILES
O=C(C=C1)N(CCCCCCN[C@H]2CC[C@@]3([H])[C@]4([H])CCC5=CC(OC)=CC=C5[C@@]4([H])CC[C@]23C)C1=O
InChi Key
LUFAORPFSVMJIW-ZRJUGLEFSA-N
InChi Code
InChI=1S/C29H40N2O3/c1-29-16-15-23-22-10-8-21(34-2)19-20(22)7-9-24(23)25(29)11-12-26(29)30-17-5-3-4-6-18-31-27(32)13-14-28(31)33/h8,10,13-14,19,23-26,30H,3-7,9,11-12,15-18H2,1-2H3/t23-,24-,25+,26+,29+/m1/s1
Chemical Name
1-(6-(((8R,9S,13S,14S,17S)-3-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione
Synonyms
U 73122; U73122; U73122.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 0.01 mg/mL warmed (0.02 mM)
Water:<1 mg/mL
Ethanol:N/A
Solubility (In Vivo)
2% Tween 80+saline: 5mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1522 mL 10.7610 mL 21.5220 mL
5 mM 0.4304 mL 2.1522 mL 4.3044 mL
10 mM 0.2152 mL 1.0761 mL 2.1522 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • U73122

    Effects of U73122 and its analog U73343 on the hydrolysis of [3H]PIP2 by PLC-β isozymes.



    U73122

    Effect of U73122 on TPA-induced ear edema in mice.J Pharmacol Exp Ther.2004 May;309(2):697-704.
  • U73122

    Effect of U73122 on IL-8- and LTB4-induced Ca2+ mobilization in human neutrophils.J Pharmacol Exp Ther.2004 May;309(2):697-704.
  • U73122

    Anti-inflammatory effects of U73122 and indomethacin on carrageenan-induced hind paw edema in rats.


    U73122

    U73122 inhibits LPS-induced PGE2 production in peritoneal lavage fluid.J Pharmacol Exp Ther.2004 May;309(2):697-704.
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