Biological Activity
Phospholipase C inhibitor. Inhibits agonist-induced platelet aggregation with IC50 values of 1-5 μM. Potently inhibits human polymorphonuclear neutrophil adhesion on biological surfaces (IC50 < 50 nM) and exhibits antinociceptive activity in vivo. Also activates TRPM4 and inhibits TRPM3 channels. Negative control U 73343 (Cat. No. 4133) also available.
Licensing Information
Sold with the permission of Pharmacia
Technical Data
| M. Wt | 464.65 |
| Formula | C29H40N2O3 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 112648-68-7 |
| PubChem ID | 104794 |
| InChI Key | LUFAORPFSVMJIW-ZRJUGLEFSA-N |
| Smiles | [H][C@]23[C@@]([C@]([H])(CC[C@@H]4NCCCCCCN5C(C=CC5=O)=O)[C@]4(C)CC3)([H])CCC1=CC(OC)=CC=C12 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility
Please refer to these solubility guidelines for U 73122 (Cat.No. 1268).
Preparing Stock Solutions
The following data is based on the product molecular weight 464.65. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.15 mL | 10.76 mL | 21.52 mL |
| 5 mM | 0.43 mL | 2.15 mL | 4.3 mL |
| 10 mM | 0.22 mL | 1.08 mL | 2.15 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
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References
References are publications that support the products' biological activity.
Bleasdale et al (1990) Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils. J.Pharmacol.Exp.Ther. 255 756 PMID: 2147038
Shi et al (2008) Phospholipase Cβ3 in mouse and human dorsal root ganglia and spinal cord is a possible target for treatment of neuropathic pain. Proc.Natl.Acad.Sci.U.S.A. 105 20004 PMID: 19066214
Smith et al (1996) U-73122: a potent inhibitor of human polymorphonuclear neutrophil adhesion on biological surfaces and adhesion-related effector functions. J.Pharmacol.Exp.Ther. 278 320 PMID: 8764366
Leitner et al (2016) Direct modulation of TRPM4 and TRPM3 channels by the phospholipase C inhibitor U73122. Br.J.Pharmacol. 173 2555 PMID: 27328745
Keywords: U 73122, supplier, Phospholipases, C, inhibitors, inhibits, PC-PLC, PI-PLC, Esterases, U73122, Phospholipases, Phospholipase, C, TRPM, Phospholipases, Tocris Bioscience
