U-73122 |
| Catalog No.GC10451 |
U-73122 is a potent and selective phospholipase C (PLC) inhibitor with an IC50 value of approximately 1-2.1µM. It also inhibits 5-lipoxygenase (5-LO).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 112648-68-7
Sample solution is provided at 25 µL, 10mM.
U-73122 is a potent and selective phospholipase C (PLC) inhibitor with an IC50 value of approximately 1-2.1µM. It also inhibits 5-lipoxygenase (5-LO)[1]. U-73122 can inhibit Ca2+ release from the intracellular sarcoplasmic reticulum by inhibiting the Ca2+ pump[2]. U-73122 is a potent inhibitor of the smooth muscle endoplasmic reticulum calcium ATPase (SERCA) pump [3].
In vitro, treatment of human osteosarcoma MG-63 cells with U-73122 (1, 10µM) for 24h reduced cell number and cell-cell adhesion, significantly changed cell morphology, and rearranged the expression group of PLC enzymes [4]. Treatment of UMR-106 cells with U-73122 (0.2-10µM) for 3min dose-dependently inhibited calcium transients stimulated by endothelin-1 and parathyroid hormone[5]. U-73122 (2-12µM) treatment of β-TC3 cells dose-dependently inhibited the effects of carbachol on intracellular free calcium and insulin release[6].
In vivo, U-73122 (9mg/kg) treated wild-type mice by intraperitoneal injection for 15min significantly reduced cardiac TNF-α expression[7].
References:
[1] Sarabia-Sánchez M A, Moreno-Londoño A P, Castañeda-Patlán M C, et al. Non-canonical Wnt/Ca2+ signaling is essential to promote self-renewal and proliferation in colon cancer stem cells[J]. Frontiers in Oncology, 2023, 13: 1121787.
[2] Macmillan D, McCarron J G. The phospholipase C inhibitor U‐73122 inhibits Ca2+ release from the intracellular sarcoplasmic reticulum Ca2+ store by inhibiting Ca2+ pumps in smooth muscle[J]. British journal of pharmacology, 2010, 160(6): 1295-1301.
[3] Hollywood M A, Sergeant G P, Thornbury K D, et al. The PI‐PLC inhibitor U‐73122 is a potent inhibitor of the SERCA pump in smooth muscle[J]. British journal of pharmacology, 2010, 160(6): 1293-1294.
[4] Lo Vasco V R, Leopizzi M, Di Maio V, et al. U-73122 reduces the cell growth in cultured MG-63 ostesarcoma cell line involving Phosphoinositide-specific Phospholipases C[J]. Springerplus, 2016, 5(1): 156.
[5] Tatrai A, Suk K L, Stern P H. U-73122, a phospholipase C antagonist, inhibits effects of endothelin-1 and parathyroid hormone on signal transduction in UMR-106 osteoblastic cells[J]. Biochimica et Biophysica Acta (BBA)-Molecular Cell Research, 1994, 1224(3): 575-582.
[6] Chen T H, Hsu W H. U-73122 inhibits carbachol-induced increases in [Ca2+] i, IP3, and insulin release in β-TC3 cells[J]. Life sciences, 1994, 56(5): 103-108.
[7] Peng T, Shen E, Fan J, et al. Disruption of phospholipase Cγ1 signalling attenuates cardiac tumor necrosis factor-α expression and improves myocardial function during endotoxemia[J]. Cardiovascular research, 2008, 78(1): 90-97.
| Cell experiment [1]: | |
Cell lines | MG-63 cells |
Preparation Method | Cells were treated with DMSO, 1μM U-73122, and 10μM U-73122 for 24 hours. PCR analysis was performed on the cells at 0, 1, 3, 6, and 24h, and morphological experiments were performed at 18 and 24 hours. |
Reaction Conditions | 1、10µM; 24h |
Applications | U-73122 treatment reduced cell number and cell-cell adhesion, significantly altered cell morphology, and rearranged the expression profile of PLC enzymes. |
| Animal experiment [2]: | |
Animal models | Wild-type mice |
Preparation Method | Wild-type mice were treated with either U-73122 or its inactive analogue U-73343 (9mg/kg, i.p.) for 15 min, followed by LPS (4mg/kg, i.p.) for 4 h. |
Dosage form | 9mg/kg; i.p. |
Applications | U-73122 significantly attenuated TNF-a mRNA expression by 70%, compared with U-73343. |
References: [1]Lo Vasco V R, Leopizzi M, Di Maio V, et al. U-73122 reduces the cell growth in cultured MG-63 ostesarcoma cell line involving Phosphoinositide-specific Phospholipases C[J]. Springerplus, 2016, 5(1): 156. [2]Peng T, Shen E, Fan J, et al. Disruption of phospholipase Cγ1 signalling attenuates cardiac tumor necrosis factor-α expression and improves myocardial function during endotoxemia[J]. Cardiovascular research, 2008, 78(1): 90-97. | |
| Cas No. | 112648-68-7 | SDF | |
| 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 | ||
| Canonical SMILES | CC12CCC3C(C1CCC2NCCCCCCN4C(=O)C=CC4=O)CCC5=C3C=CC(=C5)OC | ||
| Formula | C29H40N2O3 | M.Wt | 464.64 |
| Solubility | ≥ 5.67mg/mL in DMSO with gentle warming, ≥ 15.5mg/mL in EtOH with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1522 mL | 10.761 mL | 21.522 mL |
| 5 mM | 0.4304 mL | 2.1522 mL | 4.3044 mL |
| 10 mM | 0.2152 mL | 1.0761 mL | 2.1522 mL |
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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