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Riociguat

CAS No. 625115-55-1

Riociguat ( BAY 63-2521 | BAY63-2521 | Riociguat )

产品货号. M18919 CAS No. 625115-55-1

Riociguat 是一种鸟苷酸环化酶刺激剂,可导致血管平滑肌松弛,用于治疗严重的肺动脉高压。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥486 有现货
10MG ¥778 有现货
25MG ¥1345 有现货
50MG ¥2041 有现货
100MG ¥3499 有现货
500MG ¥7954 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    Riociguat
  • 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
    Riociguat 是一种鸟苷酸环化酶刺激剂,可导致血管平滑肌松弛,用于治疗严重的肺动脉高压。
  • 产品描述
    Riociguat, also known as BAY 63-2521, is a novel drug that is currently in clinical development by Bayer. It is a stimulator of soluble guanylate cyclase (sGC). At the moment Phase III clinical trials investigate the use of riociguat as a new approach to treat two forms of pulmonary hypertension (PH): chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension (PAH). Riociguat constitutes the first drug of a novel class of sGC stimulators.(In Vitro):[3H]Rauwolscine binding to α2 adrenergic receptor is reversible, stcreospccific, and saturable. [3H]Rauwolscine specifically labels both the high and low affinity states of the α2 adrenergic receptor in brain membranes. [3H]Rauwolscine also behaves as a 5-HT1A receptor agonist and this conclusion is compatible with earlier functional studies, indicating that rauwolscine (as well as yohimbine) has agonistic properties at the level of 5-HT autoreceptors. When using [3H]5-HT as a radioligand, rauwolscine is determined to have relatively high affinity for the human receptor (Ki human=14.3 nM, Ki rat=35.8 nM). Saturation studies shows that the affinity of [3H]Rauwolscine is similar in mouse, rat, rabbit, dog (2.33-3.03 nM) except man where it is significantly higher (0.98 nM) .
  • 体外实验
    Riocigua stimulates the recombinant sGC concentration dependently from 0.1 to 100?μM with a two-fold to 73-fold effect by an NO-independent but haem-dependent mechanism.?Riociguat inhibits platelet function in washed platelets but not in whole blood, and exerts no direct effects on contractility and relaxation of cardiac myocytes.
  • 体内实验
    Riociguat (10 mg/kg/d, p.o.) partially reverses the pulmonary arterial hypertension, the right heart hypertrophy and the structural remodelling of the lung vasculature in chronic treatment of hypoxic mice and MCT-injected rats.
  • 同义词
    BAY 63-2521 | BAY63-2521 | Riociguat
  • 通路
    Others
  • 靶点
    Other Targets
  • 受体
    Guanylate cyclase
  • 研究领域
    Cardiovascular Disease
  • 适应症
    ——

化学信息

  • CAS Number
    625115-55-1
  • 分子量
    422.42
  • 分子式
    C20H19FN8O2
  • 纯度
    >98% (HPLC)
  • 溶解度
    DMSO : ≥ 50 mg/mL; 118.37 mM
  • SMILES
    C(=O)(N(C)c1c(nc(nc1N)c1c2c(nccc2)n(n1)Cc1c(cccc1)F)N)OC
  • 化学全称
    methyl (4,6-diamino-2-(1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)pyrimidin-5-yl)(methyl)carbamate

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. Schermuly RT, et al. Eur Respir J. 2008, 32(4), 881-891.
产品手册
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