【产品介绍】：

生物活性：Riociguat-13C,d6 is the 13C and deuterium labeled Riociguat (HY-14779). Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension.
IC50 & Target：sGC[2]
体外研究(In Vitro)：Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].Riocigua 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].
德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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 in chronic treatment of hypoxic mice and MCT-injected rats[3].
德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
NCT NumberSponsorConditionStart DatePhaseNCT00454558BayerHypertension, PulmonaryJanuary 2007Phase 2NCT04062565University of ArizonaPulmonary Arterial HypertensionMarch 25, 2019Phase 3NCT02117791BayerHypertension, PulmonaryJuly 16, 2014 NCT00680654BayerHypertension, PulmonaryOctober 2008Phase 1NCT03273257International CTEPH AssociationChronic Thromboembolic Pulmonary Hypertension|CTEPHAugust 17, 2018Phase 2NCT00855465BayerPulmonary HypertensionFebruary 2009Phase 3NCT02545465BayerHypertension, PulmonarySeptember 15, 2015NCT02634203Assistance Publique - Hôpitaux de Paris|BayerChronic Thromboembolic Pulmonary HypertensionJanuary 19, 2016Not ApplicableNCT02744339Medical University of ViennaHypertension, Pulmonary|Heart Failure With Normal Ejection FractionMarch 2016Phase 2NCT04813926Bayer|Xcenda, LLCPulmonary Arterial HypertensionJuly 16, 2021NCT02170025Bayer|Merck Sharp & Dohme LLCCystic FibrosisSeptember 30, 2014Phase 2NCT03809156University of Calgary|BayerPulmonary HypertensionApril 26, 2016Phase 4NCT04366622BayerClinical PharmacologyApril 14, 2010Phase 1NCT00640315BayerHypertension, Pulmonary|Pulmonary Disease, Chronic ObstructiveAugust 2008Phase 1NCT01179334BayerPulmonary HypertensionAugust 2010Phase 2NCT00863681BayerHypertension, PulmonaryMarch 12, 2009Phase 3NCT01065051BayerHypertension, Pulmonary|Ventricular Dysfunction, LeftNovember 2010Phase 2NCT05582811Danish Headache CenterHeadacheOctober 26, 2022Not ApplicableNCT02915835Dinesh Khanna, MD, MS|Bayer|University of MichiganScleroderma|Digital UlcersSeptember 2016Phase 2NCT02159313BayerHealthy VolunteersJune 2014Phase 1NCT04600492National Hospital Organization Okayama Medical Center|Bayer Yakuhin, Ltd.Hypertension, PulmonaryOctober 16, 2020Phase 2NCT05825417Sheffield Teaching Hospitals NHS Foundation Trust|University of Glasgow|University of Sheffield|University of Newcastle Upon-Tyne|University of CambridgePulmonary Arterial HypertensionJune 14, 2023Phase 4NCT01172756BayerHypertension, Pulmonary|Ventricular Dysfunction, LeftJuly 2010Phase 2NCT02007629BayerHypertension, PulmonaryFebruary 18, 2014Phase 3NCT02633397Mark Gladwin|University of PittsburghSickle Cell DiseaseApril 11, 2017Phase 2NCT03074539Medical University of ViennaChronic Thromboembolic Pulmonary Hypertension|Sleep Disordered BreathingFebruary 1, 2017Not ApplicableNCT00855660BayerPharmacology, ClinicalMarch 2009Phase 1NCT04364464BayerClinical PharmacologyFebruary 19, 2010Phase 1NCT02625558University of CincinnatiSarcoidosisApril 2015Phase 4NCT00810693BayerPulmonary HypertensionDecember 2008Phase 3NCT03389321ActelionHealthy SubjectsJanuary 9, 2018Phase 1NCT00694850BayerHypertension, PulmonaryAugust 2, 2008Phase 2NCT02428985BayerHypertension, PulmonaryJune 29, 2015NCT01926847BayerRaynaud DiseaseOctober 2013Phase 2NCT02556268BayerHIV-DDIFebruary 23, 2016Phase 1NCT02562235Bayer|Merck Sharp & Dohme LLCHypertension, PulmonaryOctober 29, 2015Phase 3NCT05140525Dr Sudarshan Rajagopal|Actelion|Duke UniversityCTEPHSeptember 1, 2023Phase 3NCT05750446Danish Headache CenterMigraine Without AuraApril 1, 2023Not ApplicableNCT02159326BayerDrug InteractionsJune 2014Phase 1NCT04211272ActelionHealthyJanuary 14, 2020Phase 1NCT05762146Maastricht UniversityIschemic Stroke, AcuteSeptember 5, 2022Phase 2NCT02092818BayerHypertension, PulmonaryMay 31, 2014NCT02024386Richard Moon|Duke UniversityHypertension, Pulmonary|Altitude SicknessJanuary 2014Phase 4NCT01065454BayerHypertension, Pulmonary|Ventricular Dysfunction, LeftApril 14, 2010Phase 2NCT01165931BayerCoronary Artery DiseaseMay 2012Phase 2NCT02191137BayerHypertension, PulmonarySeptember 23, 2014Phase 4NCT00910429BayerPulmonary HypertensionJuly 1, 2009Phase 3NCT02283762BayerScleroderma, SystemicJanuary 15, 2015Phase 2NCT02891850BayerPulmonary Arterial HypertensionJanuary 11, 2017Phase 4NCT02138825BayerIdiopathic Interstitial Pneumonias + Hypertension,PulmonaryJune 4, 2014Phase 2NCT05339087Heidelberg University|Merck Sharp & Dohme LLCPulmonary Vascular Disorder|Primary Pulmonary Hypertension|Systemic Sclerosis|Other Systemic Involvement of Connective TissueOctober 24, 2022Phase 2NCT01489488BayerPharmacology, ClinicalJanuary 2012Phase 1NCT04954742Heidelberg University|Merck Sharp & Dohme LLCPrimary Pulmonary Arterial Hypertension|Chronic Thromboembolic Pulmonary HypertensionApril 13, 2022Phase 4
分子量：429.45
Formula：C1913CH13D6FN8O2
非标记 CAS：625115-55-1
性状：固体
颜色：White to off-white
中文名称：利奥西呱-13C,d6
运输条件：Room temperature in continental US; may vary elsewhere.
储存方式：Powder：-20°C：3 years，4°C：2 years
In solvent：-80°C：6 months，-20°C：1 month