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Riociguat Suppliers list
Company Name: Henan DaKen Chemical CO.,LTD.
Tel: +86-371-55531817
Products Intro: Product Name:Riociguat
Purity:99% Package:100g,500g,1KG,10KG,100KG
Company Name: Henan Tianfu Chemical Co.,Ltd.
Tel: 0371-55170693
Products Intro: CAS:625115-55-1
Purity:99% Package:500G;1KG;5KG;25KG
Tel: +86 21 5161 9050/ 5187 7795
Products Intro: CAS:625115-55-1
Purity:98% HPLC Package:5MG;10MG;50MG;100MG,1G,5G
Company Name: Lianyungang happen teng technology co., LTD
Tel: 15950718863
Products Intro: Product Name:riociguat
Purity:98.00% Package:1kg,10kg,50kg,100kg
Company Name: career henan chemical co
Tel: +86-371-86658258
Products Intro: Product Name:Riociguat
Purity:99% Package:1kg;2USD

Lastest Price from Riociguat manufacturers

  • Riociguat
  • US $1.00 / ASSAYS
  • 2019-10-30
  • CAS: 625115-55-1
  • Min. Order: 25ASSAYS
  • Purity: 99%
  • Supply Ability: 1ton
  • Riociguat
  • US $2.00 / kg
  • 2019-07-06
  • CAS:625115-55-1
  • Min. Order: 1kg
  • Purity: 99%
  • Supply Ability: 100kg
Riociguat Basic information
Pharmacological effects Clinical evaluation Production Method Patent cases
Product Name:Riociguat
Synonyms:Riociguat IMpurtiy D;Riocguat;Riociguat;N-[4,6-Diamino-2-[1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-pyrimidinyl]-N-methylcarbamic acid methyl ester;Bay 63-2521;Carbamic acid, (4,6-diamino-2-(1-((2-fluorophenyl)methyl)-1H-pyrazolo(3,4-B)pyridin-3-yl)-5-pyrimidinyl)methyl-, methyl ester;Riociguat, BZY 632521;Riociguat (BAY 63-2521)
Product Categories:API
Mol File:625115-55-1.mol
Riociguat Structure
Riociguat Chemical Properties
Boiling point 567.2±50.0 °C(Predicted)
density 1.51
Safety Information
MSDS Information
Riociguat Usage And Synthesis
Pharmacological effectsRiociguat is a soluble guanylyl cyclase activator, developed by the German Bayer ,it is an important signaling enzyme, which can be activated by nitric oxide (NO) to catalyze guanosine triphosphate ( GTP) to convert into the second messenger cyclic guanosine monophosphate (cGMP). Soluble guanylate cyclase is currently the only known NO receptor. Damage of NO-sGC-cGMP signal pathway is believed to be the cause of the incidence of cardiovascular, lung, endothelium, kidney and liver diseases. NO synthesis in patients with pulmonary hypertension is not enough, NO donor drugs, although effective, short half-life, riociguat can directly activate sGC, stable NO-sGC combination so as to upregulate the second messenger cGMP. riociquat can significantly increase exercise tolerance in patients with hemodynamic parameters of cardiac function and prolong the time to reach clinical worsening (PATENT study), It may also be effective in treating CTEPH(CHEST study) .
October 8, 2013, the US FDA approved Riociguat for the treatment of chronic thromboembolic pulmonary hypertension and PAH (Pulmonary Arterial Hypertension).
At present, Riociguat is not yet sold in the domestic market ,in the United States it is sold by the Haoeyou Pharmacy , the pharmacy is subsidiary of California Healthcom Group, because the market ofRiociguat is in its infancy, its sales grow slowly.
Clinical evaluationIn clinical trials ,261 patients with chronic thromboembolic pulmonary hypertension (CTEPH) were divided into riociguat and placebo groups, a six-minute walk distance (6MWD) as the main clinical endpoint, after 16 weeks of treatment, 6MWD of riociguat group increased by 46 meters higher than the average in the placebo group. 443 cases of PAH were divided into riociguat and placebo groups,after 12 weeks of treatment, riociguat group increased 36 meters higher than the average 6MWD in the placebo group. Boxed warning suggests that the drug has a embryo toxicity, pregnant patients are forbidden.
Adempas is granted baseing on two global III studies CHEST-1 and PATENT-1, whose findings are published in the July 25, 2013"New England Journal of Medicine," (2013; 369: 330-40; 2013; 369: 319-29). Thomson Reuters released analysis report that it is expected that sales of the drug in 2017 will reach $ 679 million, while the market will face a potential threat constituted by the Swiss company Actelion bosentan and Gilead drug Imber bosentan tablets.
The above information is edited by the chemicalbook of Tian Ye.
Production MethodSynthetic key of Riociguat is the synthesis of three heterocyclic ring. Compounds 1 and 2 directly close the pyrazole ring to generate 3,3 and 4 and then close the pyrazole ring to obtain5, ethyl of 5 is dehydrated using trifluoroacetic anhydride to give a cyano group after amidation by the ammonia , the cyano group is treated with methanol sodium and chloride ammonium to get amidine 6. The two nitrogen atoms on Amidine 6 as dinucleophile, with two cyano on compound 7 as the electrophile ,directly close the pyrimidine ring to give 8. pyrimidine 5-position amino group on 8 with a strong nucleophilic, directly reacts with methyl chloride and then methylates to give riociguat.
a chemical reactions road map of Riociguat production
Figure 1 is a chemical reactions road map of Riociguat production .
Patent casesUS7173037 (there is a deadline to April 25, 2023), US6743798 (valid until July 16, 2019).
DescriptionIn 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.
Chemical PropertiesBrownish Orange Solid
OriginatorBayer (Germany)
UsesRiocguat is used in the treatment for pulmonary hypertension.
DefinitionChEBI: A carbamate ester that is the methyl ester of {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamic acid. It is used for treatment of chronic thromboembolic pulmonary hypertension an pulmonary arterial hypertension
Brand nameAdempas
Riociguat Preparation Products And Raw materials
Tag:Riociguat(625115-55-1) Related Product Information
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