U-73122CAS: 112648-68-7
MF: C29H40N2O3
MW: 464.64
A phospholipase C,phospholipase A2, and 5-LO inhibitor.

U-73122 (CAS 112648-68-7)

U-73122 | CAS 112648-68-7 is rated 5.0 out of 5 by 2.
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Synonym: 1-(6-((17β-3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione
Application: A phospholipase C,phospholipase A2, and 5-LO inhibitor
CAS Number: 112648-68-7
Purity: ≥98%
Molecular Weight: 464.64
Molecular Formula: C29H40N2O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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U-73122 is an inhibitor of phospholipase C, phospholipase A2, and 5-LO (5-lipoxygenase). In neutrophils and human platelets, U-73122 inhibits agonist-induced phospholipase C (IC50=1.0-2.1 µM) activation. This compound affects the phospholipases by inhibiting the hydrolysis of PPI (phosphatidylinositol) to IP3 (inositol triphosphate), which in turn leads to a drop in cytosolic Ca2+. In SK-N-SH neuroblastoma cells, U-73122 inhibits agonist-induced down-regulation of muscarinic receptors. In addition, it is a useful tool to investigate receptor-mediated PI turnover in signal transduction. U-73122 is a potent inhibitor of human neutrophil adhesion to biological surfaces (IC50 = 50 nM) as well as adhesion-dependent granule exocytosis and oxidative burst. U-73343 (sc-201422) is useful as a negative control for investigations of U-73122 phospholipase C antagonism and its cellular consequences.


References

1. Smith, R.J., et al. 1990. J. Pharmacol. Exp. Ther. 253: 688-697. PMID: 2338654
2. Bleasdale, J.E., et al. 1990. J. Pharmacol. Exp. Ther. 255 756-768. PMID: 2147038
3. Thompson A.K., et al. 1991. J. Biol. Chem. 266: 23856-23862. PMID: 1660886
4. Yule, D.I., et al. 1992. J. Biol. Chem. 267: 13830-13835. PMID: 1629184
5. Smith, R.J., et al. 1996. J. Pharmacol. Exp. Ther. 278: 320-329. PMID: 8764366

Usage :
U-73122 is only sparingly soluble in aqueous media. Because of this U-73122 can only be delivered to the cell by forming a complex with serum proteins or by dissolving it with an organic solvent.
Preparation of Working Solutions:
1. Dissolve U-73122 in Dichloromethane (sc-239703) or Chloroform (sc-239527).
2. Aliquot amount needed for a single experiemnt into suitable vials.
3. Evaporate the methylene chloride or chloroform using nitrogen.
4. The result is a film of U-73122 that can be dissolved in DMSO (5mM), ethanol (2mM in 100%) or an aqueous medium that contains serum or serum albumin (1-10 mg/mL), which forms a complex with U-73122, thus eliminating the need to use an organic solvent to deliver the compound to the cells.
Useful Range of Concentrations:
Useful concentrations of U-73122 range between 0.1 and 10 µM. Several factors affect the necessary concentration including: cell density, cell type, medium concentration and the particular variable that is being measured.
Physical State :
Solid
Solubility :
Soluble in anhydrous DMSO (1 mg/ml), DMF, PBS pH7.2, anhydrous Chloroform (3 mg/ml), anhydrous Ethanol (500 µg/ml), dichloromethane, and aqueous solutions (sparingly). Insoluble in water.
Storage :
Store at room temperature
Melting Point :
121-122° C
Boiling Point :
617.14° C at 760 mmHg (Predicted)
Density :
1.17 g/cm3 (Predicted)
Refractive Index :
n20D 1.59 (Predicted)
IC50 :
Recombinant enzyme: IC50 = 30 nM; Neutrophil Elastase: IC50 = 50 nM (human); Parathyroid hormone-induced Ca2+ transients: IC50 = 0.5 µM; Platelet aggregation induced by collagen: IC50 = 0.6 µM; ET-1 hormone-induced Ca2+ transients: IC50 = 0.8 µM; PMNL homogenates: IC50 = 2.4 µM; Platelet aggregation induced by thrombin : IC50 = 5 µM; HIV-1 integrase: IC50 = 7 µM
pK Values :
pKb: 10.69 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
5631
SMILES :
CC12CCC3C(C1CCC2NCCCCCCN4C(=O)C=CC4=O)CCC5=C3C=CC(=C5)OC

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Certificate of Analysis

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U-73122  Product Citations

See how others have used U-73122. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 24 total

PMID: # 30206934  Tantilertanant, Y.|Niyompanich, J.|Everts, V.|Supaphol, P.|Pavasant, P.|Sanchavanakit, N.| et al. 2019. J. Cell. Physiol. 234: 4528-4539.

PMID: # 29251630  Leung, CS.|Yeung, TL.|Yip, KP.|Wong, KK.|Ho, SY.|Mangala, LS.|Sood, AK.|Lopez-Berestein, G.|Sheng, J.|Wong, ST.|Birrer, MJ.|Mok, SC.| et al. 2018. J. Clin. Invest. 128: 589-606.

PMID: # 30103900  Sharapova, TN.|Romanova, EA.|Sashchenko, LP.|Yashin, DV.| et al. 2018. Biochimie. 152: 174-180.

PMID: # 27189756  Do Van, B.|Gouel, F.|Jonneaux, A.|Timmerman, K.|Gelé, P.|Pétrault, M.|Bastide, M.|Laloux, C.|Moreau, C.|Bordet, R.|Devos, D.|Devedjian, JC.| et al. 2016. Neurobiol. Dis. 94: 169-78.

PMID: # 26673139  Galindo-Villegas, J. et al. 2016. J. Immunol. 196: 738-49.

PMID: # 27127172  Kamranvar, SA. et al. 2016. Oncotarget. 7: 30820-30.

PMID: # 27746193  Gao, J.|Bai, T.|Ren, L.|Ding, Y.|Zhong, X.|Wang, H.|Guo, Y.|Li, J.|Liu, Y.|Zhang, Y.| et al. 2016. Peptides. 86: 72-79.

PMID: # 26925647  Akekawatchai, C. et al. 2016. Asian Pac. J. Cancer Prev. 17: 581-90.

PMID: # 26185418  Khan, N. et al. 2015. Drug design, development and therapy. 9: 3497-506.

PMID: # 24357048  Luo, XP. et al. 2014. Cell biochemistry and function. 32: 294-8.

Citations 1 to 10 of 24 total

What should the product be stored in once in solution in DMSO or ethanol?

Asked by: 13punMA
Thank you for your question about our product U-73122 (CAS# 112648-68-7). DMSO is probably better overall for long term storage.
Answered by: Chemical Support 8
Date published: 2017-03-17

What is the desired solvent for this chemical?

Asked by: 13punMA
Thank you for your question about our product U-73122 (CAS# 112648-68-7). This product is slightly soluble in DMSO up to (2mg/ml) or 100% ethanol (1mg/ml) .
Answered by: Chemical Support 8
Date published: 2017-03-17
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Rated 5 out of 5 by from Good Good.
Date published: 2015-10-05
Rated 5 out of 5 by from Santagata Santagata, et. al. (PubMed ID 11375483) found that this specific PLC inhibitor provided an almost complete impedes acetylcholine-induced nuclear translocation of tubby-AChR-M1 double transfectants in the presence of acetylcholine. -SCBT Publication Review
Date published: 2015-04-11
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