Riociguat

Catalog No.S8135 Batch:S813503

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Technical Data

Formula

C20H19FN8O2
Molecular Weight 422.42 CAS No. 625115-55-1
Solubility (25°C)* In vitro DMSO 84 mg/mL (198.85 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.25mg/ml 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. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.25mg/ml 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. 
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Riociguat is an oral soluble guanylate cyclase (GC) stimulator, used in the treatment of ipulmonary hypertension.
Targets
guanylate cyclase [1]
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]

Protocol (from reference)

Animal Study:[1]
  • Animal Models

    Chronic hypoxic mice, and monocrotaline (MCT)-injected rats

  • Dosages

    10 mg/kg

  • Administration

    p.o.

Selleck's Riociguat has been cited by 9 publications

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

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.