
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)






规格 | 价格/人民币 | 库存 | 数量 |
5MG | ¥486 | 有现货 |
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10MG | ¥778 | 有现货 |
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25MG | ¥1345 | 有现货 |
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50MG | ¥2041 | 有现货 |
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100MG | ¥3499 | 有现货 |
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500MG | ¥7954 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称Riociguat
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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
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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。
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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) .
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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.
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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.
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同义词BAY 63-2521 | BAY63-2521 | Riociguat
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通路Others
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靶点Other Targets
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受体Guanylate cyclase
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研究领域Cardiovascular Disease
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适应症——
化学信息
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CAS Number625115-55-1
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分子量422.42
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分子式C20H19FN8O2
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纯度>98% (HPLC)
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溶解度DMSO : ≥ 50 mg/mL; 118.37 mM
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SMILESC(=O)(N(C)c1c(nc(nc1N)c1c2c(nccc2)n(n1)Cc1c(cccc1)F)N)OC
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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
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储存条件(-20℃)
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运输条件With Ice Pack
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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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