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BQ-788 Sale

目录号 : GC35546

A peptide ETB receptor antagonist

BQ-788 Chemical Structure

Cas No.:173326-37-9

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产品描述

BQ-788 is a peptide endothelin type B (ETB) receptor antagonist (IC50 = 1.2 nM).1 It is selective for ETB over ETA receptors (IC50 = 280 nM), as well as angiotensin, calcitonin, or neuropeptide receptors at 10 ?M. 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).2 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.3 BQ-788 also attenuates delayed hypotension, vascular hyporeactivity to norepinephrine, and hepatocellular injury and dysfunction in a rat model of LPS-induced endotoxemia.4

1.Okada, M., and Nishikibe, M.BQ-788, a selective endothelin ETB receptor antagonistCardiovasc. Drug Rev.20(1)53-66(2002) 2.Ishikawa, K., Ihara, M., Noguchi, K., et al.Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788Proc. Natl. Acad. Sci. USA91(11)4892-4896(1994) 3.?ugowska-Umer, H., Umer, A., Kuziemski, K., et al.The protective effect of endothelin receptor antagonists against surgically induced impairment of gastrointestinal motility in ratsJ. Smooth Muscle Res.5523-33(2019) 4.Ruetten, H., and Thiemermann, C.Effect of selective blockade of endothelin ETB receptors on the liver dysfunction and injury caused by endotoxaemia in the ratBr. J. Pharmacol.119(3)479-486(1996)

Chemical Properties

Cas No. 173326-37-9 SDF
Canonical SMILES CCCC[C@H](C(O)=O)NC([C@@H](CC1=CN(C(OC)=O)C2=CC=CC=C12)NC([C@H](CC(C)(C)C)NC(N3[C@H](C)CCC[C@@H]3C)=O)=O)=O
分子式 C34H51N5O7 分子量 641.8
溶解度 Soluble in DMSO 储存条件 Store at -20°C,protect from light
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1 mM 1.5581 mL 7.7906 mL 15.5812 mL
5 mM 0.3116 mL 1.5581 mL 3.1162 mL
10 mM 0.1558 mL 0.7791 mL 1.5581 mL
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Research Update

BQ-788, a selective endothelin ET(B) receptor antagonist

Cardiovasc Drug Rev 2002 Winter;20(1):53-66.PMID:12070534DOI:10.1111/j.1527-3466.2002.tb00082.x.

We describe characteristics of a selective endothelin (ET) ET(B) receptor antagonist, BQ-788 [N-cis-2,6-dimethylpiperidinocarbonyl-L-gamma-methylleucyl-D-1-methoxycarbonyltryptophanyl-D-norleucine], which is widely used to demonstrate the role of endogenous or exogenous ETs in vitro and in vivo. In vitro, BQ-788 potently and competitively inhibited (125)I-labeled ET-1 binding to ET(B) receptors in human Girrardi heart cells (hGH) with an IC(50) of 1.2 nM, but only poorly inhibited the binding to ET A receptors in human neuroblastoma cell line SK-N-MC cells (IC(50), 1300 nM). In isolated rabbit pulmonary arteries, BQ-788 showed no agonistic activity up to 10 microM and competitively inhibited the vasoconstriction induced by an ET(B)-selective agonist (pA(2), 8.4). BQ-788 also inhibited several bioactivities of ET-1, such as bronchoconstriction, cell proliferation, and clearance of perfused ET-1. Thus, it is confirmed that BQ-788 is a potent, selective ET(B) receptor antagonist. In vivo, in conscious rats, BQ-788, 3 mg/kg/h, i.v., completely inhibited a pharmacological dose of ET-1- or sarafotoxin6c (S6c) (0.5 nmol/kg, i.v.)-induced ET(B) receptor-mediated depressor, but not pressor responses. Furthermore, BQ-788 markedly increased the plasma concentration of ET-1, which is considered an index of potential ET(B) receptor blockade in vivo. In Dahl salt-sensitive hypertensive (DS) rats, BQ-788, 3 mg/kg/h, i.v., increased blood pressure by about 20 mm Hg. It is reported that BQ-788 also inhibited ET-1-induced bronchoconstriction, tumor growth and lipopolysaccharide-induced organ failure. These data suggest that BQ-788 is a good tool for demonstrating the role of ET-1 and ET(B) receptor subtypes in physiological and/or pathophysiological conditions.

Transdermal BQ-788/EA@ZnO quantum dots as targeting and smart tyrosinase inhibitors in melanocytes

Mater Sci Eng C Mater Biol Appl 2019 Sep;102:45-52.PMID:31147016DOI:10.1016/j.msec.2019.04.042.

Tyrosinase inhibitors could effectively limit the activity of tyrosinase in melanocytes to reduce the excessive synthesis and deposition of melanin. However, low skin permeability and lacking in targeting greatly restricted their application. Herein, ZnO quantum dots were synthesized by gel-sol method and grafted with BQ-788, which have been employed as transdermal and targeting carrier to delivery ellagic acid to melanocytes. Ellagic acid loaded ZnO quantum dots with the size distribution of around 9 nm could targetedly bind to melanocytes and enter the melanocytes by endocytosis within 1 h. The ellagic acid release behavior was controlled by the decreasing of pH via the rapid dissolution of ZnO. When the concentration of BQ-788/EA@ZnO was 12.5 μg/mL, the inhibition rate on tyrosinase activity and melanin deposition were up to 44.23 ± 4.97% and 37.50 ± 5.23%, respectively. In view of their good biocompatibility, they were of great potential in clinically external application for tyrosinase inhibition.

Effects of BQ-788 on amitriptyline-induced cardiovascular toxicity

Hum Exp Toxicol 2013 Mar;32(3):316-22.PMID:22653689DOI:10.1177/0960327112446819.

Objective: We investigated both the effects of the endothelin type B (ETB) receptor antagonist, BQ-788, on amitriptyline-induced cardiotoxicity and the role of ETB receptors on amitriptyline-induced cardiovascular depression. Methods: Male Wistar rats were anaesthetized with urethane/chloralose. Mean arterial pressure (MAP), heart rate (HR) and QRS duration were recorded. Toxicity was induced by amitriptyline infusion (0.94 mg/kg per min) until the 50% inhibition of MAP. In the first protocol, 5% dextrose or BQ-788 bolus was administered to control or experimental group animals, respectively. In the second protocol, after incubation with BQ-788 or 5% dextrose, amitriptyline was infused. Results: Amitriptyline caused a significant decrease in MAP, prolonged QRS duration and decreased HR for both the groups. BQ-788 administration improved MAP (5, 10 and 15 min), shortened the prolonged QRS (5 and 10 minutes) and increased HR (5, 10 and 15 min) compared with dextrose group. While all the amitriptyline-infused rats survived in BQ-788 group, all the amitriptyline-infused rats died within 20 min in dextrose group. In the second protocol, BQ-788 incubation did not cause any statistically significant change in amitriptyline-induced cardiovascular depression. Conclusion: BQ-788 may have beneficial effects in amitriptyline-induced cardiovascular changes via a physiologic antagonism. ETB receptor antagonists may be the promising antidotes for the cardiovascular toxicity with hypotension and bradycardia.

Synergistic inhibition by BQ-123 and BQ-788 of endothelin-1-induced contractions of the rabbit pulmonary artery

Br J Pharmacol 1994 Oct;113(2):336-8.PMID:7834180DOI:10.1111/j.1476-5381.1994.tb16901.x.

In the rabbit isolated pulmonary artery, neither the ETA receptor antagonist, BQ-123 (10 microM), nor the ETB receptor antagonist, BQ-788 (10 microM), inhibited the contractions induced by 1 nM endothelin-1 (ET-1). However, the combination of BQ-123 and BQ-788 completely inhibited the ET-1-induced contraction. In contrast, the ETB-selective agonist, sarafotoxin S6c (1 nM)-induced contraction was completely inhibited by BQ-788 but not by BQ-123. In receptor binding assays, [125I]-ET-1 specific binding to pulmonary arterial membranes was inhibited by BQ-123 (1 microM) by approximately 20% and additive treatment with BQ-788 (1 microM) completely inhibited the BQ-123-resistant component of [125I]-ET-1 specific binding. The present study demonstrates synergistic inhibition by BQ-123 and BQ-788 of ET-1-induced contraction of the rabbit pulmonary artery and the coexistence of ETA and ETB receptors, suggesting that the activation of either only ETA or only ETB receptors may be sufficient to cause complete vasoconstriction. Therefore, blockade of both receptor subtypes would be necessary for the inhibition of some ETA/ETB composite types of responses.

Novel antagonist of endothelin ETB1 and ETB2 receptors, BQ-788: effects on blood vessel and small intestine

Biochem Biophys Res Commun 1994 Nov 30;205(1):168-73.PMID:7999018DOI:10.1006/bbrc.1994.2645.

The effects of a peptide, BQ-788 [N-cis-2, 6-dimethyl-piperidinocarbonyl-L-gamma-methylleucyl-D-1- methoxycarbonyltryptophanyl-D-norleucine], on isolated blood vessel and small intestine were examined. In the rat aorta, BQ-788 antagonized the endothelium-dependent, ETB1 receptor-mediated relaxation due to endothelin (ET)-3 with EC50 of 3 microM. In the rat aorta without endothelium, 10 microM BQ-788 weakly antagonized the ETA1-mediated contractile effects of ET-1 and ET-3. In the rabbit saphenous vein, it has been shown that ETA1, ETA2, ETB1 and ETB2 receptors mediate contraction. BQ-788 (10 microM) almost completely inhibited the contractile effect of sarafotoxin S6c (an ETB1 and ETB2 agonist). BQ-788 also antagonized the contractile effect of ET-3 (an ETA1, ETB1 and ETB2 agonist) more strongly than desensitization of ETB1 and ETB2 receptors. However, BQ-788 did not antagonize the effect of ET-1 (agonist of all four receptors). In the guinea pig ileum, 10 microM BQ-788 completely inhibited the relaxation mediated by ETB1 and ETB2 receptors. These results suggest that BQ-788 is a novel antagonist of ETB1 and ETB2 receptors with weak antagonistic effect on the ETA1 receptor.