Riociguat

製品コードS8135 バッチS813503

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 DMSO 84 mg/mL (198.85 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 4.250mg/ml (10.06mM) Taking the 1 mL working solution as an example, add 50 μL of 85 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.250mg/ml (0.59mM) Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/18550612/
  • https://pubmed.ncbi.nlm.nih.gov/26282717/
  • https://pubmed.ncbi.nlm.nih.gov/26407652/

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：

Assessing the role of endothelium-protective drugs: Functional and molecular insights into chronic thromboembolic pulmonary hypertension derived endothelial cells [ Biomed Pharmacother, 2025, 190:118425] PubMed: 40763482
Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805] PubMed: 39581704
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
Serum from Men with the Severe Form of COVID‐19 Impairs the Nitric Oxide Signaling Pathway in Isolated Corpus Cavernosum from Mice: An In Vitro Study [ Andrologia, 2023, 10.1155/2023/9059973] PubMed: None
Serum from Men with the Severe Form of COVID-19 Impairs the Nitric Oxide Signaling Pathway in Isolated Corpus Cavernosum from Mice: An In Vitro [ Andrologia, 2023, 13 pages] PubMed: None
TRP'ing on-a-chip: therapeutically targeting TRPC6 and advanced in vitro glomerular modelling [ Radbound Repository, 2023, 229 p] PubMed: none
Фармакологические эффекты нового стимулятора растворимой гуанилатциклазы при экспериментальной легочной артериальной гипертензии [ Fundamental medicine , 2023 , 22(1):14-22] PubMed: None
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

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。