BMS 182874 hydrochloride

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Cat.No. 1441 - BMS 182874 hydrochloride | C17H19N3O3S.HCl | CAS No. 1215703-04-0
Description: Highly selective, orally active non-peptide ETA antagonist
Chemical Name: 5-(Dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Literature

Biological Activity

Potent, selective and competitive non-peptide endothelin ETA receptor antagonist (Ki = 48 nM). Displays > 1000-fold selectivity over ETB 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

SolubilitySoluble 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.

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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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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 ETA receptor antagonist. J.Pharmacol.Exp.Ther. 272 1124 PMID: 7891325


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

2 Citations for BMS 182874 hydrochloride

Citations are publications that use Tocris products. Selected citations for BMS 182874 hydrochloride include:

Yuan et al (2015) Endothelial cells enhance the migration of bovine meniscus cells. Arthritis Rheumatol 67 182 PMID: 25307081

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


Do you know of a great paper that uses BMS 182874 hydrochloride from Tocris? If so please let us know.

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