Product Details
| Product Name:
BQ-788 |
CAS No.:
173326-37-9 |
| Purity:
98.67% |
Supply Ability:
10g |
| Release date:
2024/11/13 |
Product Introduction
Bioactivity
| 名稱 | BQ-788 |
| 描述 | 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. |
| 體外活性 | BQ-788 potently and competitively inhibits the binding of (125I-labeled ET-1) to ETB receptors in human Girardi heart cells (hGH) with an IC50 of 1.2 nM, but poorly inhibits the binding to ETA receptors in human neuroblastoma cells (SK-N-MC) with an IC50 of 1300 nM. Up to 10 μM, BQ-788 shows no agonistic activity and competitively inhibits vasoconstriction induced by an ETB-selective agonist (pA2, 8.4). Additionally, BQ-788 inhibits several bioactivities of ET-1, including bronchoconstriction, cell proliferation, and clearance of perfused ET-1[1]. |
| 體內(nèi)活性 | 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]. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 150 mg/mL (233.72 mM), Sonication is recommended.
|
| 關(guān)鍵字 | BQ 788 | BQ-788 |
| 相關(guān)產(chǎn)品 | Macitentan | BMS 182874 | Bosentan | BMS 182874 hydrochloride | Sitaxsentan sodium | Edonentan | Sulfisoxazole | Ambrisentan | Sparsentan | Aprocitentan | Nebentan potassium | Clazosentan |
| 相關(guān)庫(kù) | 疼痛相關(guān)化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 膜蛋白靶向化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 已知活性化合物庫(kù) | GPCR靶點(diǎn)分子庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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