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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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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. 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.
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].
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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].
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Animal Protocol |
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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 |
Molecular Formula |
C29H40N2O3
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Molecular Weight |
464.64
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CAS # |
112648-68-7
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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
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InChi Key |
LUFAORPFSVMJIW-ZRJUGLEFSA-N
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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
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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
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Synonyms |
U 73122; U73122; U73122.
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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)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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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.
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.
(2) Be sure to add the solvent(s) in order.