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Submit ReviewSR 140333
Description: Potent NK1 antagonist
Chemical Name: 1-[2-[(3S)-3-(3,4-Dichlorophenyl)-1-[2-[3-(1-methylethoxy)phenyl]acetyl]-3-piperidinyl]ethyl]-4-phenyl-1-azoniabicyclo[2.2.2]octane chloride
Purity: ≥97% (HPLC)
Biological Activity for SR 140333
SR 140333 is a potent NK1 receptor antagonist (Ki = 0.74 nM. IC50 = 1.6 nM). Inhibits substance P-invoked calcium mobilization and outward current (IC50 = 1.3 nM); blocks NK1-mediated nitric oxide-dependent vasodilation in vivo.
Compound Libraries for SR 140333
SR 140333 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for SR 140333
| M. Wt | 656.12 |
| Formula | C37H45Cl3N2O2 |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 153050-21-6 |
| PubChem ID | 108166 |
| InChI Key | NQHFSECYQAQZBN-LSYPWIJNSA-M |
| Smiles | O=C(N2C[C@@](CC[N+]3(CC5)CCC(C4=CC=CC=C4)5CC3)([C@]6=CC=C(Cl)C(Cl)=C6)CCC2)CC1=CC(OC(C)C)=CC=C1.[Cl-] |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SR 140333
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 65.61 | 100 | |
| ethanol | 65.61 | 100 |
Preparing Stock Solutions for SR 140333
The following data is based on the product molecular weight 656.12. Batch specific molecular weights may vary from batch to batch due to the degree 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 | 1.52 mL | 7.62 mL | 15.24 mL |
| 5 mM | 0.3 mL | 1.52 mL | 3.05 mL |
| 10 mM | 0.15 mL | 0.76 mL | 1.52 mL |
| 50 mM | 0.03 mL | 0.15 mL | 0.3 mL |
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Product Datasheets for SR 140333
References for SR 140333
References are publications that support the biological activity of the product.
Hall and Brain (1994) Inhibition by SR140333 of NK1 tachykinin receptor-evoked, nitric oxide-dependent vasodilation in the hamster cheek pouch microvasculature in vivo. Br.J.Pharmacol. 113 522 PMID: 7530573
Nieuwmeyer et al (2006) Ava[L-Pro9,N-MeLeu10] substance P(7-11) (GR 73632) and Sar9, Met(O2)11 increase distention-induced peristalsis through activation of neurokinin-1 receptors on smooth muscle and interstitial cells of Caj J.Pharmacol.Exp.Ther. 317 439 PMID: 16330493
Oury-Donat et al (1994) SR 140333, a novel, selective, and potent nonpeptide antagonist of the NK1 tachykinin receptor: characterization on the U373MG cell line. J.Neurochem. 62 1399 PMID: 7510780
Emonds-Alt et al (1993) In vitro and in vivo biological activities of SR140333, a novel non-peptide tachykinin NK1 receptor antagonist. Eur.J.Pharmacol. 250 403 PMID: 7509286
If you know of a relevant reference for SR 140333, please let us know.
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Keywords: SR 140333, SR 140333 supplier, SR140333, neurokinin1, nk1, tachykinins, receptor, antagonists, potent, NK1, Receptor, 4012, Tocris Bioscience
1 Citation for SR 140333
Citations are publications that use Tocris products. Selected citations for SR 140333 include:
Xinzhong et al (2019) A Mast-Cell-Specific Receptor Mediates Neurogenic Inflammation and Pain. Neuron 101 412-420.e3 PMID: 30686732
Do you know of a great paper that uses SR 140333 from Tocris? Please let us know.
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Literature in this Area
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