U-73122
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.
- 1. Chien-Liang Liu, Shih-Ping Cheng, et al. "Quinolinate Phosphoribosyltransferase Promotes Invasiveness of Breast Cancer Through Myosin Light Chain Phosphorylation." Front Endocrinol (Lausanne). 2021 Feb 4;11:621944. PMID: 33613454 2. Zhou J, Lai W, et al. "BLT1 in dendritic cells promotes Th1/Th17 differentiation and its deficiency ameliorates TNBS-induced colitis." Cell Mol Immunol. 2018 Apr 18. PMID:29670278
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 464.64 |
| Cas No. | 112648-68-7 |
| Formula | C29H40N2O3 |
| Solubility | insoluble in H2O; ≥15.5 mg/mL in EtOH with gentle warming and ultrasonic; ≥5.67 mg/mL in DMSO with gentle warming |
| Chemical Name | 1-[6-[[(8R,9S,13S,14S,17S)-3-methoxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl]amino]hexyl]pyrrole-2,5-dione |
| SDF | Download SDF |
| Canonical SMILES | CC12CCC3C(C1CCC2NCCCCCCN4C(=O)C=CC4=O)CCC5=C3C=CC(=C5)OC |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
Human neutrophils |
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Reaction Conditions |
15 min or 3 h incubation |
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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] | |
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Animal models |
Male Sprague-Dawley rats, ~ 200 g |
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Dosage form |
30 mg/kg Administered intraperitoneally (i.p.) |
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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. |
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Note |
The technical data provided above is for reference only. |
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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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