Shelf life (days): 1460.0
Formulation: A solid
Formal Name: N-[4,6-diamino-2-[1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-pyrimidinyl]-N-methyl-13C-d3-carbamic acid, methyl ester
Purity: ≥99% deuterated forms (d1-d3)
Formula Markup: C19[13C]H16D3FN8O2
Formula Weight: 426.4
CAS Number: 2749393-44-8
Notes: Riociguat-13C-d3 is intended for use as an internal standard for the quantification of riociguat (Item No. 9000554) by GC- or LC-MS. 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 and 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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