化合物 BQ-788|T10595|TargetMol

BQ-788
173326-37-9

￥1230 1mg 起订

￥1730 2mg 起订

￥2680 5mg 起订

上海更新日期：2024-09-30

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 BQ-788

英文名称：: BQ-788

CAS号：: 173326-37-9

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 98.67%

产品类别：: 抑制剂

货号：: T10595

Product Introduction

Bioactivity

Name	BQ-788
Description	BQ-788 is a selective and potent ETB receptor antagonist with potential hypertensive activity.BQ-788 inhibits ET-1 binding to ETB receptors and inhibits exogenous ET-1-induced elevation of coronary artery perfusion pressure.
In vitro	BQ-788 potently and competitively inhibits the binding of 125I-labeled ET-1 to ETB receptors in human Girrardi heart cells (hGH) with an IC50 of 1.2 nM. However, it poorly inhibits the binding to ETA receptors in the human neuroblastoma cell line SK-N-MC cells (IC50, 1300 nM). BQ-788, up to 10 μM, shows no agonistic activity and competitively inhibits the vasoconstriction induced by an ETB-selective agonist (pA2, 8.4). Additionally, BQ-788 inhibits several bioactivities of ET-1, such as bronchoconstriction, cell proliferation, and clearance of perfused ET-1[1].
In vivo	In conscious rats, BQ-788 (3 mg/kg/h, i.v.) completely inhibits ETB receptor-mediated depressor responses induced by a pharmacological dose of ET-1 or sarafotoxin6c (0.5 nmol/kg, i.v.), but not pressor responses. Additionally, BQ-788 markedly increases the plasma concentration of ET-1, considered an index of potential ETB receptor blockade in vivo. In Dahl salt-sensitive hypertensive (DS) rats, BQ-788 (3 mg/kg/h, i.v.) raises blood pressure by about 20 mm Hg. It is reported that BQ-788 also inhibits ET-1-induced bronchoconstriction, tumor growth, and lipopolysaccharide-induced organ failure[1]. BQ 788 (3 mg/kg) results in an eightfold leftward shift in the ET-1 dose-response curve, suggesting significant involvement of ETB dilator receptors[2]. In mice treated with 30 nmol BQ-788 by intraplantar administration, there is a reduction in mechanical hyperalgesia (47% and 42%), thermal hyperalgesia (68% and 76%), oedema (50% and 30%), myeloperoxidase activity (64% and 32%), and overt-pain like behaviors. Additionally, intraplantar treatment with clazosentan or BQ-788 decreases spinal (45% and 41%) and peripheral (47% and 47%) superoxide anion production as well as spinal (47% and 47%) and peripheral (33% and 54%) lipid peroxidation, respectively[3].
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	DMSO : 150 mg/mL (233.72 mM), Sonication is recommended.
Keywords	BQ 788 \| BQ-788
Inhibitors Related	Clazosentan \| Aprocitentan \| SB-209670 \| Edonentan \| Sparsentan \| Sulfisoxazole \| Macitentan \| BMS 182874 \| BMS 182874 hydrochloride \| Ambrisentan \| Bosentan \| Sitaxsentan sodium
Related Compound Libraries	Bioactive Compound Library \| Bioactive Compounds Library Max \| GPCR Compound Library \| Membrane Protein-targeted Compound Library \| Pain-Related Compound Library \| Drug Repurposing Compound Library

BQ788|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	(12年)
注册资本	566.265100万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,工厂,试剂,定制,服务
主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务