SR 140333

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Cat.No. 4012 - SR 140333 | C37H45Cl3N2O2 | CAS No. 153050-21-6
Description: Potent NK1 receptor 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)
Datasheet
Citations
Literature

Biological Activity

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

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Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 65.61 100
ethanol 65.61 100

Preparing Stock Solutions

The following data is based on the product molecular weight 656.12. 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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: SR 140333, supplier, SR140333, neurokinin1, nk1, tachykinins, receptor, antagonists, potent, NK1, Receptor, Tocris Bioscience

Citations for SR 140333

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