Formulation: A solid
Formal Name: N-[(cis-2,6-dimethyl-1-piperidinyl)carbonyl]-4-methyl-L-leucyl-1-(methoxycarbonyl)-D-tryptophyl-D-norleucine
Purity: ≥90%
Formula Markup: C34H51N5O7
Formula Weight: 641,8
Shelf life (days): 1460
CAS Number: 173326-37-9
Notes: BQ-788 is a peptide endothelin type B (ETB) receptor antagonist (IC50 = 1.2 nM).{64228} It is selective for ETB over ETA receptors (IC50 = 280 nM), as well as angiotensin, calcitonin, or neuropeptide receptors at 10 µM. BQ-788 inhibits calcium mobilization induced by endothelin-1 (ET-1) in human Girrardi heart cells (IC50 = 0.54 nM) and vasoconstriction induced by the ETB-selective agonist BQ-3020 in isolated rat pulmonary arteries (pA2 = 8.4).{28374} In vivo, BQ-788 (1 mg/kg, i.v.) inhibits ET-1-induced depressor responses and induces pressor responses in rats. It protects against laparotomy and surgical gut handling-induced inhibition of intestinal motility in rats.{64229} BQ-788 also attenuates delayed hypotension, vascular hyporeactivity to norepinephrine, and hepatocellular injury and dysfunction in a rat model of LPS-induced endotoxemia.{64230}
English
Deutsch
