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Tocris/BMS 182874 hydrochloride/1441/50/50 mg

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货号: 1441/50

品牌: Tocris

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Description: Highly selective, orally active non-peptide ET_A antagonist

Chemical Name: 5-(Dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide hydrochloride

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent, selective and competitive non-peptide endothelin ET_A receptor antagonist (K_i = 48 nM). Displays > 1000-fold selectivity over ET_B receptors. Inhibits ET-1-induced pressor response following oral or intravenous administration in vivo. Inhibits ET-1-induced longitudinal muscle contraction in the mouse colon in vitro.

Licensing Information

Sold with the permission of Bristol-Myers Squibb Company, subject to U.S. Patent No. 5,378,715 and other US and foreign patents

Compound Libraries

BMS 182874 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	381.88
Formula	C₁₇H₁₉N₃O₃S.HCl
Storage	Store at RT
Purity	≥98% (HPLC)
CAS Number	1215703-04-0
PubChem ID	56972163
InChI Key	UZZFRNZGYDOBAO-UHFFFAOYSA-N
Smiles	Cl.CN(C)C1=C2C=CC=C(C2=CC=C1)S(=O)(=O)NC1=C(C)C(C)=NO1

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

Solubility	Soluble to 100 mM in DMSO

Solubility

Soluble to 100 mM in DMSO

Preparing Stock Solutions

The following data is based on the product molecular weight 381.88. 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	2.62 mL	13.09 mL	26.19 mL
5 mM	0.52 mL	2.62 mL	5.24 mL
10 mM	0.26 mL	1.31 mL	2.62 mL
50 mM	0.05 mL	0.26 mL	0.52 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Khan et al (2006) Pharmacological characterization of endothelin receptors-mediated contraction in the mouse isolated proximal and distal colon. Br.J.Pharmacol. 147 607 PMID: 16432510

Stein et al (1994) The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(Dimethylamino)-N-(3,4-dimethyl-5-isoazolyl)-1-naphthalenesulfonamide. J.Med.Chem. 37 329 PMID: 8308857

Webb et al (1995) BMS-182874 is a selective, nonpeptide endothelin ET_A receptor antagonist. J.Pharmacol.Exp.Ther. 272 1124 PMID: 7891325

Keywords: BMS 182874 hydrochloride, supplier, selective, orally, active, non-peptide, ETA, antagonists, receptors, endothelin, BMS182874, hydrochloride, Endothelin, ETA, Receptors, Endothelin, ETA, Receptors, Tocris Bioscience

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