| Identification | Back Directory | [Name]
5-(DIMETHYLAMINO)-N-(3,4-DIMETHYL-5-ISOXAZOLYL)-1-NAPHTHALENESULFONAMIDE HYDROCHLORIDE | [CAS]
153042-42-3 | [Synonyms]
BMS182874HCl
BMS 182874 HYDROCHLORIDE
5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide
1-Naphthalenesulfonamide, 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-
5-(DIMETHYLAMINO)-N-(3,4-DIMETHYL-5-ISOXAZOLYL)-1-NAPHTHALENESULFONAMIDE HYDROCHLORIDE | [Molecular Formula]
C17H19N3O3S | [MDL Number]
MFCD06795832 | [MOL File]
153042-42-3.mol | [Molecular Weight]
345.42 |
| Chemical Properties | Back Directory | [Boiling point ]
524.5±60.0 °C(Predicted) | [density ]
1.332±0.06 g/cm3(Predicted) | [storage temp. ]
Store at RT | [form ]
Solid | [pka]
7?+-.0.50(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
BMS 182874 Hydrochloride, is a potent, selective, and competitive non-peptide endothelin ETAR antagonist (Ki = 48 nM). ET-A receptors are predominantly detected in peripheral tissues, especially in vascular smooth muscle tissues where they mediate vasoconstriction. | [Definition]
ChEBI: 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide is a member of naphthalenes and a sulfonic acid derivative. | [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. | [in vivo]
BMS 182874 (100 μM/kg, p.o.; a single oral) makes arterial pressure slowly fell by 25% from a control level. After dosing for 12 and 24 h makes arterial pressure is still 12% below the control level[1].
| Animal Model: | Kidney Deoxycorticosterone acetate -salt hypertensive rats[1] | | Dosage: | 100 μM/kg | | Administration: | Oral gavage (p.o.); Intravenous injection (i.v.) | | Result: | Made arterial pressure slowly fell by 25% from a control level. After dosing for 12 and 24 h, makes arterial pressure is still 12% below the control level.
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| [IC 50]
ETA: 0.15 μM (IC50); ETA: 0.055 μM (Ki) |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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