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ABT-546 (A-216546) is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is >25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively[1]. | [in vivo]
ABT-546 (A-216546; 0-100 mg/kg; oral administration; for 1 hour or 4 hours; male Sprague-Dawley rats) treatment dose-dependently blocks endothelin-1-induced pressor response in conscious rats[1]. | Animal Model: | Male Sprague-Dawley rats (250-350 g) induced with endothelin-1[1] | | Dosage: | 0.1 mg/kg, 1 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg | | Administration: | Oral administration; for 1 hour or 4 hours | | Result: | Exhibited a dose-dependent inhibition of the peak pressor response to endothelin-1, and statistically significant inhibition was achieved at doses of 3 to 100 mg/kg.
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| [IC 50]
ETA: 0.46 nM (Ki) | [References]
[1] u-Wong JR, et al. Pharmacology of A-216546: a highly selective antagonist for endothelin ET(A) receptor. Eur J Pharmacol. 1999 Feb 5;366(2-3):189-201. DOI:10.1016/s0014-2999(98)00891-7 |
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BOC Sciences
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1-631-485-4226; 16314854226 |
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MedChemExpress
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www.medchemexpress.com |
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