Riociguat

製品コードS8135 バッチS813502

印刷

化学情報

Chemical Structure Synonyms BAY 63-2521 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H19FN8O2
分子量 422.42 CAS No. 625115-55-1
Solubility (25°C)* 体外  
 
 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

生物活性

製品説明 Riociguat is an oral soluble guanylate cyclase (GC) stimulator, used in the treatment of ipulmonary hypertension.
in vitro BAY 63-2521 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. [1] Riociguat inhibits platelet function in washed platelets but not in whole blood, and exerts no direct effects on contractility and relaxation of cardiac myocytes. [2] [3]
in vivo In chronic treatment of hypoxic mice and MCT-injected rats, 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. [1]

プロトコル(参考用のみ)

動物実験 動物モデル Chronic hypoxic mice, and monocrotaline (MCT)-injected rats
投薬量 10 mg/kg
投与方法 p.o.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Activating NO-sGC crosstalk in the mouse vascular niche promotes vascular integrity and mitigates acute lung injury [ J Exp Med, 2023, 220(2)e20211422] PubMed: 36350314
Optogenetic manipulation of cyclic guanosine monophosphate to probe phosphodiesterase activities in megakaryocytes [ Open Biol, 2022, 12(8):220058] PubMed: 35975649
Single-cell transcriptomic analysis reveals a hepatic stellate cell-activation roadmap and myofibroblast origin during liver fibrosis [ Hepatology, 2021, 10.1002/hep.31987] PubMed: 34089528
Repurposing Riociguat to Target a Novel Paracrine Nitric Oxide-TRPC6 Pathway to Prevent Podocyte Injury [ Int J Mol Sci, 2021, 22(22)12485] PubMed: 34830371
Soluble guanylate cyclase stimulator reduced the gastrointestinal fibrosis in bleomycin-induced mouse model of systemic sclerosis [ Arthritis Res Ther, 2021, 23(1):133] PubMed: 33941248
Novel Targets in a High-Altitude Pulmonary Hypertension Rat Model Based on RNA-seq and Proteomics [ Front Med (Lausanne), 2021, 8:742436] PubMed: 34805208
Endothelial Sash1 Is Required for Lung Maturation through Nitric Oxide Signaling. [ Cell Rep, 2019, 27(6):1769-1780] PubMed: 31067462
TMPRSS2-ERG activates NO-cGMP signaling in prostate cancer cells. [ Oncogene, 2019, 38(22):4397-4411] PubMed: 30718921
Non-canonical AR activity facilitates endocrine resistance in breast cancer. [ Endocr Relat Cancer, 2019, 26(2):251-264] PubMed: 30557851

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。