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Tocris/SR 140333/4012/10/10 mg

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货号: 4012/10

品牌: Tocris

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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)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent NK₁ receptor antagonist (K_i = 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

SR 140333 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

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.

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

Product Datasheets

Certificate of Analysis / Product Datasheet

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

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

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