MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

BQ-788 sodium salt

CAS No. : 156161-89-6

产品活性：BQ-788 sodium salt is a potent and selective ETB receptor antagonist, inhibiting ET-1 binding to ETB receptors with an IC₅₀ of 1.2 nM in human Girrardi heart cells.

研究领域：GPCR/G Protein

作用靶点：Endothelin Receptor

In Vitro: BQ-788 potently and competitively inhibits ¹²⁵I-labeled ET-1 binding to ETB receptors in human Girrardi heart cells with an IC₅₀ of 1.2 nM, but only poorly inhibits the binding to ETA receptors in human neuro-blastoma cell line SK-N-MC cells (IC₅₀, 1300 nM). BQ-788 shows no agonistic activity up to 10 μM and competitively inhibits thevasoconstriction induced by an ETB-selective agonist (pA2, 8.4). BQ-788 also inhibits several bioactivities of ET-1, such as bronchoconstriction, cell proliferation, and clearance of perfused ET-1.

In Vivo: BQ-788 (3 mg/kg/h, i.v.) completely inhibits a pharmacological dose of ET-1- or sarafotoxin6c (0.5 nmol/kg, i.v.)-induced ETB receptor-mediated depressor, but not pressor responses in conscious rats. Furthermore, BQ-788 markedly increases the plasma concentration of ET-1, which is 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.) increases blood pressure by about 20 mm Hg. It is reported that BQ-788 also inhibits ET-1-induced bronchoconstriction, tumor growth and lipopolysaccharide-induced organfailure. BQ 788 (3 mg/kg) results in an eightfold leftward shift in the ET-1 dose-response curve, suggesting a significant involvement of ETB dilator receptors. Mice are treated with 30 nmol BQ-788 by intraplantar, reduce mechanical hyperalgesia (47% and 42%), thermal hyperalgesia (68% and 76%), oedema (50% and 30%); myeloperoxidase activity (64% and 32%), and overt-pain like behaviours. 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.

相关产品：Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Peptidomimetic Library  |  BQ-788  |  [Asn18] Endothelin-1, human  |  TBC3711  |  BQ-3020 TFA  |  Sparsentan  |  [Lys4] Sarafotoxin S6c  |  Nebentan potassium  |  Bosentan  |  Endothelin 1 (swine, human) (TFA)  |  Ambrisentan  |  Ro 46-2005  |  [Ala2] Endothelin-3, human  |  ZD-1611  |  PD-159020  |  Aminaftone  |  A-192621  |  Macitentan  |  Sulfisoxazole  |  Endothelin-3, human, mouse, rabbit, rat TFA  |  IRL 2500  |  Carperitide acetate  |  Atrial Natriuretic Peptide (ANP) (1-28), rat TFA  |  ACT-373898  |  Kendomycin  |  Zibotentan  |  BQ-123 TFA

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种*仅有化合物库，我们致力于为*科研客户提供前沿的高品质小分子活性化合物；
•   50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种顶级期刊及制药 Patent 收录了MCE客户的科研成果；
•   专业团队跟踪新的制药及生命科学研究进展，为您提供*新的活性化合物；
•   与世界各大制药公司及*科研机构建立了长期的合作。