L-733060 hydrochloride
Based on 1 publication(s) in Google Scholar
L-733060 hydrochloride is a selective neurokinin-1 (NK-1) receptor antagonist. L-733060 hydrochloride mainly regulates pain transmission and neural plasticity by blocking the binding of Substance P (P substance) to the NK-1 receptor. L-733060 hydrochloride blocks the promoting effect of Substance P on long-term potentiation (LTP) in the hippocampus. L-733060 hydrochloride reverses the orofacial hyperalgesia induced by experimental occlusal interference (EOI) in rats. L-733060 hydrochloride hydrochloride inhibits neurogenic plasma extravasation at a dose that does not cause adverse cardiovascular effects in rodents, and also acts as an anti-tumor agent. L-733060 hydrochloride can be used for the study of chronic orofacial pain.
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- Pureté: 99.9%
- CAS No.: 148687-76-7
- Formule: C20H20ClF6NO
- Masse moléculaire:439.82
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) L-733060 hydrochloride
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Activité biologique
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NK1R |
L-733060 (30-300 nM) inhibits the [Ca2+]i mobilisation caused by substance P (100 nM) in a concentration-dependent manner in human tachykinin NK1 receptor-transfected CHO cells[1].
L-733060 (2.5-20 μM; 48 and or 96 h) results in a concentration-dependent cytotoxicity in COLO 858 cells[2].
L-733060 (10-30 μM; 24 and 48 h) inhibits MEL H0 cells proliferation with IC50s of 27.5 μM and 18.9 μM at 24 h and 48 h, respectively[2].
L-733060 (20-50 μM; and or 72 h) inhibits COLO 679 cells growth with IC50s of 33.8 μM and 31.5 μM at 30 h and 72 h, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:COLO 858 cells
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Concentration:2.5, 5, 10, 20 μM
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Incubation Time:0, 48, 96 h
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Result:Inhibited cells growth with IC50s of 8.7 μM and 7.1 μM at 48 h and 96 h, respectively.
L-733060 (300-3000 μg/kg; i.v.) has no significant hypotensive or bradycardic effects are observed at doses of <3000 μg/kg in conscious or anaesthetised rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (200 g) with electrical stimulation of the trigeminal ganglion[1]
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Dosage:10, 100, 1000 mg/kg
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Administration:I.v. injection
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Result:Produced a significant dose-related inhibition of plasma extravasation with an ID50 of 212±19 μg/kg.
Chemical Information
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CAS No. 148687-76-7
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Appearance Solid
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Masse moléculaire 439.82
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Formule C20H20ClF6NO
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Color White to off-white
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SMILES
FC(F)(C1=CC(C(F)(F)F)=CC(CO[C@@H]2[C@@](C3=CC=CC=C3)([H])NCCC2)=C1)F.Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
2025 Mar 31;16(1):3093. PMID: 40164597
Solvant et solubilité
H2O : 22 mg/mL (50.02 mM; Need warming)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Seabrook GR, et, al. L-733,060, a novel tachykinin NK1 receptor antagonist; effects in [Ca2+]i mobilisation, cardiovascular and dural extravasation assays. Eur J Pharmacol. 1996 Dec 12; 317(1):129-35. [Content Brief]
[2]. Muñoz M, et, al. Antitumoral action of the neurokinin-1 receptor antagonist L-733 060 on human melanoma cell lines. Melanoma Res. 2004 Jun;14(3):183-8. [Content Brief]
[3]. SI-Yi Mo et al. Neuronal Activities in the Rostral Ventromedial Medulla Associated with Experimental Occlusal Interference-Induced Orofacial Hyperalgesia. J Neurosci. 2022 Jul 6;42(27):5314-5329. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.2737 mL | 11.3683 mL | 22.7366 mL | 56.8414 mL |
| 5 mM | 0.4547 mL | 2.2737 mL | 4.5473 mL | 11.3683 mL | |
| 10 mM | 0.2274 mL | 1.1368 mL | 2.2737 mL | 5.6841 mL | |
| 15 mM | 0.1516 mL | 0.7579 mL | 1.5158 mL | 3.7894 mL | |
| 20 mM | 0.1137 mL | 0.5684 mL | 1.1368 mL | 2.8421 mL | |
| 25 mM | 0.0909 mL | 0.4547 mL | 0.9095 mL | 2.2737 mL | |
| 30 mM | 0.0758 mL | 0.3789 mL | 0.7579 mL | 1.8947 mL | |
| 40 mM | 0.0568 mL | 0.2842 mL | 0.5684 mL | 1.4210 mL | |
| 50 mM | 0.0455 mL | 0.2274 mL | 0.4547 mL | 1.1368 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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