What is the Riociguat?

Riociguat is , while it's Molecular Formula is C 20 H 19 FN 8 O 2 . Riociguat is used in the treatment for pulmonary hypertension.

What is the CAS number for Riociguat?

The CAS number of Riociguat is 625115-55-1.

What is Riociguat (625115-55-1) used for?

In September 2013, Health Canada approved riociguat (also referred to as BAY 63-2521), for the treatment of patients with chronic thromboembolic pulmonary hypertension (CTEPH) after surgical treatment or inoperable CTEPH and for the treatment of adults with pulmonary arterial hypertension (PAH). Riociguat has a dual mode of action and works by (a) sensitizing sGC to the body’s NO by stabilizing NO–sGC binding and (b) an NO-independent, direct stimulation of sGC via a different binding site. This process restores the NO–sGC–cGMP pathway and leads to increased generation of cGMP with subsequent vasodilation.Headache, dizziness, dyspepsia/gastritis, nausea, diarrhea, hypotension, vomiting, anemia, gastroesophageal reflux, and constipation were the most common adverse events ( 3%) observed during riociguat clinical trials. Riociguat comes with a black box warning for embryo-fetal toxicity.

What is the Riociguat?

Riociguat is , while it's Molecular Formula is C 20 H 19 FN 8 O 2 . Riociguat is used in the treatment for pulmonary hypertension.

What is the CAS number for Riociguat?

The CAS number of Riociguat is 625115-55-1.

What is Riociguat (625115-55-1) used for?

In September 2013, Health Canada approved riociguat (also referred to as BAY 63-2521), for the treatment of patients with chronic thromboembolic pulmonary hypertension (CTEPH) after surgical treatment or inoperable CTEPH and for the treatment of adults with pulmonary arterial hypertension (PAH). Riociguat has a dual mode of action and works by (a) sensitizing sGC to the body’s NO by stabilizing NO–sGC binding and (b) an NO-independent, direct stimulation of sGC via a different binding site. This process restores the NO–sGC–cGMP pathway and leads to increased generation of cGMP with subsequent vasodilation.Headache, dizziness, dyspepsia/gastritis, nausea, diarrhea, hypotension, vomiting, anemia, gastroesophageal reflux, and constipation were the most common adverse events ( 3%) observed during riociguat clinical trials. Riociguat comes with a black box warning for embryo-fetal toxicity.

Product Class

625115-55-1

Product Name：Riociguat
Molecular Formula：C₂₀H₁₉FN₈O₂
Purity：99%
Molecular Weight：422.422

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Product Details:

CasNo： 625115-55-1

Molecular Formula： C₂₀H₁₉FN₈O₂

Buy High Grade Top Purity Riociguat 625115-55-1 with Best Price

Molecular Formula:C₂₀H₁₉FN₈O₂
Molecular Weight:422.422
Boiling Point:567.202 °C at 760 mmHg
PKA:1.51±0.50(Predicted)
Flash Point:296.833 °C
PSA：138.80000
Density:1.513 g/cm³
LogP:2.95400

Riociguat(Cas 625115-55-1) Usage

Description	Riociguat, sold under the brand name Adempas, is a soluble guanylate cyclase (sGC) stimulator. Riociguat is approved for treating inoperable CTEPH or persistent/recurrent CTEPH after pulmonary endarterectomy. CTEPH occurs when blood clots block or narrow the arteries in the lungs, leading to high blood pressure and strain on the heart. By improving blood flow through vasodilation, riociguat helps alleviate these symptoms. Hangzhou Huarong Pharm Co., Ltd. established since 2009 , has been always focusing on supplying products and services to our clients in the field of small molecule drug. Huarong Pharm adheres to our vision, our mission, and our value, keeping abreast of the current trend and state-of-the-art science and technologies of the global biopharmaceutical industry to serve our clients to the utmost satisfaction. Our goal is to become a world-class leading company to support life science innovation and manufacturing.
Category	Soluble Guanylate Cyclase (sGC) Stimulator Pulmonary Hypertension Therapy
Uses	Riociguat enhances the activity of soluble guanylate cyclase (sGC), an enzyme that responds to nitric oxide (NO). By stimulating sGC both independently of NO and by enhancing NO’s effect, it increases the synthesis of cyclic guanosine monophosphate (cGMP). This leads to vasodilation of the pulmonary arteries, improved blood flow, and a reduction in pulmonary vascular resistance. It is prescribed for the treatment of two forms of pulmonary hypertension (PH): chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension (PAH). It works by stimulating the production of cyclic guanosine monophosphate (cGMP), which helps relax the blood vessels in the lungs, thereby improving blood flow and reducing the workload on the heart.

625115-55-1 Relevant articles

Riociguat for the treatment of pulmonary hypertension

Ralph T Schermuly,Wiebke Janssen,Norbert Weissmann,Johannes-Peter Stasch,Friedrich Grimminger &Hossein Ardeschir Ghofrani

Expert Opinion on Investigational Drugs Volume 20, 2011 - Issue 4

This review will help readers understand the mechanism of action of the soluble guanylate cyclase (sGC) stimulator riociguat (BAY 63-2521) and will provide a comprehensive summary regarding efficacy and safety of this drug in the management of PH. The most relevant publications up to December 2010 were used as sources for this review.

Stimulation of soluble guanylyl cyclase (sGC) by riociguat attenuates heart failure and pathological cardiac remodelling

Julia Rüdebusch, Alexander Benkner, Neetika Nath, Lina Fleuch, Lars Kaderali, Karina Grube, Karin Klingel, Gertrud Eckstein, Thomas Meitinger, Jens Fielitz, Stephan B. Felix

, British Journal of Pharmacology, Volume179, Issue11 Themed Issue: cGMP Signalling in Cell Growth and Survival June 2022 Pages 2430-2442

We hypothesized that stimulation of sGC by the sGC stimulator riociguat prevents pathological cardiac remodelling and heart failure in response to chronic pressure overload. Transverse aortic constriction or sham surgery was performed in C57BL/6N mice. After 3 weeks of transverse aortic constriction when heart failure was established, animals receive either riociguat or its vehicle for 5 additional weeks. Cardiac function was evaluated weekly by echocardiography.

625115-55-1 Process route

: 1702271-98-4
2-{1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl}-5-N-methylpyrimidine-4,5,6-triamine

: 79-22-1
methyl chloroformate

: 625115-55-1
Riociguat

Conditions

Conditions	Yield
2-{1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl}-5-N-methylpyrimidine-4,5,6-triamine; methyl chloroformate; In isopropyl alcohol; at 40 ℃; for 5h; With triethylamine; In methanol; at 45 ℃; for 1h; Temperature;	89%
With triethylamine; In dimethyl sulfoxide; at 80 ℃; for 3h; Reagent/catalyst; Temperature;	85%
With pyridine; In N,N-dimethyl-formamide; at 0 - 5 ℃; for 0.5h; Temperature;	60%
2-{1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl}-5-N-methylpyrimidine-4,5,6-triamine; With sodium carbonate; In tetrahydrofuran; water; at 0 - 5 ℃; for 0.333333h; methyl chloroformate; In tetrahydrofuran; water; at 0 - 15 ℃; for 4h;	5 g

: 6642-30-4
methyl N-methylcarbamate

: 2-{1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl}-5-iodopyrimidine-4,6-diamine

: 625115-55-1
Riociguat