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Bosentan

CAS No. 147536-97-8

Bosentan ( Ro 47-0203 )

产品货号. M12035 CAS No. 147536-97-8

Bosentan 是 ET-A 和 ET-B 的内皮素 (ET) 受体拮抗剂,Ki 分别为 4.7 nM 和 95 nM。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
25MG ¥413 有现货
50MG ¥599 有现货
100MG ¥1045 有现货
200MG ¥1758 有现货
500MG ¥2649 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    Bosentan
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    Bosentan 是 ET-A 和 ET-B 的内皮素 (ET) 受体拮抗剂,Ki 分别为 4.7 nM 和 95 nM。
  • 产品描述
    Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.(In Vitro):Bosentan (BOS) competitively and specifically antagonizes binding of 125I-labelled ET-1 to ETA receptors on human smooth muscle cells (SMC) and ETB receptors on human placenta cells. The in vitro binding affinity of Bosentan to ETA receptors on human SMC is 4.7 nM and to ETB receptors on human SMC or placenta cells is 41 or 95 nM. Bosentan has 67-fold greater selectivity for ETA than ETB receptors (mean IC50=7.1 vs 474.8 nM) in an in vitro 125I-labeling assay.(In Vivo):Single-dose Bosentan 62.5 mg significantly (p<0.01 vs baseline) plasma ET-1 levels by 2-fold in 7 pts with WHO class II or III idiopathic or CTD-associated PAH, with peak levels achieved at 8 h. In hypertensive rats, Macitentan 30 mg/kg further decreases mean arterial blood pressure (MAP) by 19 mm Hg when given on top of Bosentan 100 mg/kg. Conversely, Bosentan given on top of Macitentan fails to induce an additional MAP decrease. In pulmonary hypertensive rats, Macitentan 30 mg/kg further decreases mean pulmonary artery pressure (MPAP) by 4 mm Hg on top of Bosentan, whereas a maximal effective dose of Bosentan given on top of Macitentan does not cause any additional MPAP decrease.
  • 体外实验
    Bosentan (BOS) competitively and specifically antagonizes binding of 125I-labelled ET-1 to ETA receptors on human smooth muscle cells (SMC) and ETB receptors on human placenta cells. The in vitro binding affinity of Bosentan to ETA receptors on human SMC is 4.7 nM and to ETB receptors on human SMC or placenta cells is 41 or 95 nM. Bosentan has 67-fold greater selectivity for ETA than ETB receptors (mean IC50=7.1 vs 474.8 nM) in an in vitro 125I-labeling assay.
  • 体内实验
    In hypertensive rats, Macitentan 30 mg/kg further decreases mean arterial blood pressure (MAP) by 19 mm Hg when given on top of Bosentan 100 mg/kg. Conversely, Bosentan given on top of Macitentan fails to induce an additional MAP decrease. In pulmonary hypertensive rats, Macitentan 30 mg/kg further decreases mean pulmonary artery pressure (MPAP) by 4 mm Hg on top of Bosentan, whereas a maximal effective dose of Bosentan given on top of Macitentan does not cause any additional MPAP decrease.
  • 同义词
    Ro 47-0203
  • 通路
    GPCR/G Protein
  • 靶点
    Endothelin Receptor
  • 受体
    ET-A| ET-B
  • 研究领域
    Cardiovascular Disease
  • 适应症
    ——

化学信息

  • CAS Number
    147536-97-8
  • 分子量
    551.61
  • 分子式
    C27H29N5O6S
  • 纯度
    >98% (HPLC)
  • 溶解度
    DMSO:100 mg/mL (181.28 mM); Ethanol:3 mg/mL (5.43 mM); Water:<1 mg/mL (<1 mM)
  • SMILES
    COC1=CC=CC=C1OC1=C(NS(=O)(=O)C2=CC=C(C=C2)C(C)(C)C)N=C(N=C1OCCO)C1=NC=CC=N1 |c:4,6,10,18,20,27,29,38,40,t:2,16,36|
  • 化学全称
    ——

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1. Serafim KG, et al. naunyn Schmiedebergs Arch Pharmacol. 2015 Nov;388(11):1211-21.
产品手册
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