153042-42-3 Usage
Description
5-(DIMETHYLAMINO)-N-(3,4-DIMETHYL-5-ISOXAZOLYL)-1-NAPHTHALENESULFONAMIDE HYDROCHLORIDE, also known as BMS 182874 Hydrochloride, is a potent, selective, and competitive non-peptide endothelin ETA receptor antagonist with a Ki value of 48 nM. It is a pharmaceutical compound that has been developed for its potential therapeutic applications, particularly in the treatment of various medical conditions related to the endothelin system.
Uses
Used in Pharmaceutical Industry:
5-(DIMETHYLAMINO)-N-(3,4-DIMETHYL-5-ISOXAZOLYL)-1-NAPHTHALENESULFONAMIDE HYDROCHLORIDE is used as a therapeutic agent for the treatment of conditions related to endothelin ETA receptor overactivity. Its high selectivity and potency make it a promising candidate for the development of new drugs targeting endothelin-mediated diseases.
Used in Cardiovascular Applications:
In the cardiovascular industry, 5-(DIMETHYLAMINO)-N-(3,4-DIMETHYL-5-ISOXAZOLYL)-1-NAPHTHALENESULFONAMIDE HYDROCHLORIDE is used as a vasoconstriction modulator. It targets the endothelin ETA receptors, which are predominantly found in vascular smooth muscle tissues. By blocking these receptors, it can help in the management of conditions characterized by abnormal vasoconstriction, such as hypertension and certain heart diseases.
Used in Research and Development:
5-(DIMETHYLAMINO)-N-(3,4-DIMETHYL-5-ISOXAZOLYL)-1-NAPHTHALENESULFONAMIDE HYDROCHLORIDE is also used as a research tool in the field of endothelin receptor pharmacology. Its high affinity and selectivity for the ETA receptor make it a valuable compound for studying the role of endothelin in various physiological and pathological processes, as well as for the development of new drugs targeting the endothelin system.
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 . In vitro inhibits ET-1-induced longitudinal muscle contraction in the mouse colon.
Check Digit Verification of cas no
The CAS Registry Mumber 153042-42-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,5,3,0,4 and 2 respectively; the second part has 2 digits, 4 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 153042-42:
(8*1)+(7*5)+(6*3)+(5*0)+(4*4)+(3*2)+(2*4)+(1*2)=93
93 % 10 = 3
So 153042-42-3 is a valid CAS Registry Number.
InChI:InChI=1/C17H19N3O3S/c1-11-12(2)18-23-17(11)19-24(21,22)16-10-6-7-13-14(16)8-5-9-15(13)20(3)4/h5-10,19H,1-4H3
153042-42-3Relevant articles and documents
HALOGEN SUBSTITUTION AT THE ISOXAZOLE RING ENHANCES THE ACTIVITY OF N-(ISOXAZOLYL)SULFONAMIDE ENDOTHELIN ANTAGONISTS
Chan, Ming Fai,Raju, B.,Kois, Adam,Castillo, Rosario S.,Verner, Erik J.,et al.
, p. 2393 - 2398 (2007/10/03)
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Discovery and structure-activity relationships of sulfonamide ET(A)- selective antagonists
Stein,Floyd,Bisaha,Dickey,Girotra,Gougoutas,Kozlowski,Lee,Liu,Malley,McMullen,Mitchell,Moreland,Murugesan,Serafino,Webb,Zhang,Hunt
, p. 1344 - 1354 (2007/10/02)
Random screening of compounds in an ETA receptor binding assay led to the discovery of a class of benzenesulfonamide ligands. Optimization led to the development of 5-amino-N-(3,4-dimethyl-5-isoxazolyl)-1- naphthalenesulfonamides which were functional ant
