A potent

BQ-788 (sodium salt) – 1 mg

Brand:
Cayman
CAS:
156161-89-6
Storage:
-20
UN-No:
Non-Hazardous - /

The endothelin (ET) family of proteins mediate a variety of responses, with ET-1 being a potent and long-lasting constrictor of human cardiovascular vessels.{28375} These proteins activate the G protein-coupled receptors ETA and ETB, with ETB being non-specific for ET protein form.{28375} BQ-788 is a potent, selective antagonist of ETB (IC50 = 1.2 nM for blocking ET-1 binding to human Girardi heart cells).{28374} It weakly inhibits the binding of ET-1 to ETA receptors on human neuroblastoma SK-N-MC cells (IC50 = 1300 nM).{28374} BQ-788 competitively antagonizes the vasoconstriction induced by an ETB-selective agonist on isolated rabbit pulmonary arteries, blocks ET-1 induced bronchoconstriction in guinea pigs, and abolishes an ET-1 mediated depressor response in rats.{28374}  

 

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Description

A potent, selective antagonist of ETB (IC50 = 1.2 nM for blocking ET-1 binding to human Girardi heart cells); competitively antagonizes the vasoconstriction induced by an ETB-selective agonist on isolated rabbit pulmonary arteries

Formal name: N-[[(2R,6S)-2,6-dimethyl-1-piperidinyl]carbonyl]-4-methyl-L-leucyl-1-(methoxycarbonyl)-D-tryptophyl-D-norleucine, monosodium salt

Synonyms: 

Molecular weight: 664.8

CAS: 156161-89-6

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Vasculature|Vasodilation

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