A stimulator of sGC; stimulates recombinant sGC in a concentration-dependent manner in vitro by up to 73-fold at 100 μM or by up to 112-fold when used in combination with DEA NONOate; has no effect on phosphodiesterases PDE1-9 and PDE11 at ≤3 μM; reduces pulmonary and systemic arterial pressure at 1 and 10 mg/kg in a rabbit model of acute PAH induced by U-46619; inhibits increases in right ventricular systolic pressure

Riociguat – 50 mg

Brand:
Cayman
CAS:
625115-55-1
Storage:
-20
UN-No:
Non-Hazardous - /

Riociguat is a stimulator of soluble guanylate cyclase (sGC).{36864},{26751} It stimulates recombinant sGC in a concentration-dependent manner in vitro by up to 73-fold when used at a concentration of 100 μM or by up to 112-fold when used in combination with the nitric oxide (NO) donor DEA NONOate (Item No. 82100).{36864} It has no effect on phosphodiesterases PDE1-9 and PDE11 when used at concentrations up to 3 μM. Riociguat (1 and 10 mg/kg) reduces pulmonary and systemic arterial pressure in a rabbit model of acute pulmonary arterial hypertension (PAH) induced by U-46619 (Item No. 16450). It also inhibits increases in right ventricular systolic pressure, right heart hypertrophy, and pulmonary artery muscularization in hypoxia-induced mouse and monocrotaline-injected rat models of chronic PAH when administered at a dose of 10 mg/kg. Formulations containing riociguat have been used in the treatment of chronic thromboembolic pulmonary hypertension (CTEPH) and PAH.  

 

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SKU: 9000554 - 50 mg Category:

Description

A stimulator of sGC; stimulates recombinant sGC in a concentration-dependent manner in vitro by up to 73-fold at 100 μM or by up to 112-fold when used in combination with DEA NONOate; has no effect on phosphodiesterases PDE1-9 and PDE11 at ≤3 μM; reduces pulmonary and systemic arterial pressure at 1 and 10 mg/kg in a rabbit model of acute PAH induced by U-46619; inhibits increases in right ventricular systolic pressure, right heart hypertrophy, and pulmonary artery muscularization in hypoxia-induced mouse and monocrotaline-injected rat models of chronic PAH at 10 mg/kg

Formal name: N-[4,6-diamino-2-[1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-pyrimidinyl]-N-methyl-carbamic acid, methyl ester

Synonyms:  BAY 63-2521

Molecular weight: 422.4

CAS: 625115-55-1

Purity: ≥98%

Formulation: A crystalline solid

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