1215703-04-0

Basic information

• Product Name: N-(3,4-Dimethyl-5-isoxazolyl)-5-(dimethylamino)-1-naphthalenesulfonamide hydrochloride
• Synonyms: BMS182874;N-(3,4-Dimethyl-5-isoxazolyl)-5-(dimethylamino)-1-naphthalenesulfonamide hydrochloride
• CAS NO: 1215703-04-0
• Molecular Formula: C17H20ClN3O3S
• Molecular Weight: 381.877
• Mol File: 1215703-04-0.mol
• Article Data: 0

Chemical Properties

• Appearance: white to beige/
• Storage Temp.: 2-8°C
• Solubility: DMSO: soluble5mg/mL, clear (warmed)
• CAS DataBase Reference: N-(3,4-Dimethyl-5-isoxazolyl)-5-(dimethylamino)-1-naphthalenesulfonamide hydrochloride(CAS DataBase Reference)
• NIST Chemistry Reference: N-(3,4-Dimethyl-5-isoxazolyl)-5-(dimethylamino)-1-naphthalenesulfonamide hydrochloride(1215703-04-0)
• EPA Substance Registry System: N-(3,4-Dimethyl-5-isoxazolyl)-5-(dimethylamino)-1-naphthalenesulfonamide hydrochloride(1215703-04-0)

Safety Data

• Hazard Codes: Xn
• Statements: 22
• WGK Germany: 3
• Hazardous Substances Data: 1215703-04-0(Hazardous Substances Data)

Usage

Biological Activity

ki: 61 nm for eta in vsm-a10 cells; 48 nm for eta in cho cellsendothelin (et) was originally identified as a potent vasoactive substance secreted by endothelial cells that stimulated force development in isolated pig coronary arteries. et-1 belongs to a family of highly conserved 21-amino-acid peptides produced in numerous tissues including the lung, kidney, eye, gut and central nervous system. bms-182874 is a low molecular weight, nonpeptide endothelin (el) receptor antagonist.

in vitro

bms-182874 competitively inhibited the binding of [125i]et-1 to eta receptors in rat vascular smooth muscle a10 (vsm-a10) cell membranes (ki = 61 nm) and in cho cells stably expressing the human eta receptor (ki = 48 nm), but was a weak inhibitor at etb receptors (ki > 50 μm) and non-et receptors. bms-l 82874 inhibited et-l -stimulated inositol phosphate accumulation (kb 75 nm) and calcium mobilization (ki = 140 nm) without suppressing the maximal responses in vsm-a10 cells [1].

in vivo

when administered either orally (ed50 = 30 μmol/kg) or intravenously (ed50 = 24 μmol/kg) to conscious, normotensive rats, bms-182874 blunted the pressor response to exogenous et-l . these data demonstrate that bms-l 82874 is a competitive, selective and orally active eta receptor antagonist [1].

references

[1] maria l webb, j. eileen bird, eddie c. k. liu, patricia m. rose, randy serafino, philip d. stein and suzanne moreland. bms-182874 is a selective, nonpeptide endothelin eta receptor antagonist. jpet 272:1124-1134, 1995.