SB-209670 is a highly potent non-peptide antagonist of the endothelin (ET) receptor, exhibiting subnanomolar affinity with Ki values of 0.2 nM for ETA and 18 nM for ETB. This compound effectively inhibits the binding of 125I-labeled ET-1 to both human ET receptor subtypes, making it a valuable tool in cardiovascular and neurological research. SB-209670 demonstrates significant biological activity by reducing blood pressure in hypertensive models, offering neuroprotective effects against ischemia-induced neuronal degeneration, and inhibiting neointima formation following carotid artery balloon angioplasty in rats.
SB-209670 is a highly potent non-peptide antagonist of the endothelin (ET) receptor, exhibiting subnanomolar affinity with Ki values of 0.2 nM for ETA and 18 nM for ETB. This compound effectively inhibits the binding of 125I-labeled ET-1 to both human ET receptor subtypes, making it a valuable tool in cardiovascular and neurological research. SB-209670 demonstrates significant biological activity by reducing blood pressure in hypertensive models, offering neuroprotective effects against ischemia-induced neuronal degeneration, and inhibiting neointima formation following carotid artery balloon angioplasty in rats.
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