Riociguat, supplied by MedChemExpress, used in various techniques. Bioz Stars score: 94/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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1) Product Images from "A shear-dependent NO-cGMP-cGKI cascade in platelets acts as an auto-regulatory brake of thrombosis"
Article Title: A shear-dependent NO-cGMP-cGKI cascade in platelets acts as an auto-regulatory brake of thrombosis
Journal: Nature Communications
Figure Legend Snippet: NO-GC activity is regulated by fluid shear stress and lowers the intracellular Ca 2+ concentration. FRET/cGMP imaging of cGi500-expressing platelet thrombi formed on collagen was performed under flow on (500 s −1 ) and off (0 s −1 ) conditions. a – c Thrombi were exposed to a DEA/NO (100 nM), b SPER/NO (500 nM), or c DETA/NO (10 μM). At the end of each experiment, 20 μM ODQ was applied in the presence of the respective NO donor and continuous flow. d – f Thrombi were superfused with the NO-GC stimulators d BAY 41-2272 (5 µM) or e riociguat (5 µM), or f with the NO-GC activator cinaciguat (100 nM). g DEA/NO (100 nM)-induced cGMP signals in the presence of the MRP4 inhibitor, MK-571 (1 µM). Data are shown as mean ± SEM ( n = 18 thrombi in a , b , g ; n = 10 thrombi in c , d ; n = 15 thrombi in e , f ). h Western blot analysis of NO-GC β1, cGKI, and PECAM-1 in cytosolic and membrane fractions of mouse platelets. Data are shown as mean ± SEM ( n = 4). i Simultaneous imaging of cGMP (green trace) and Ca 2+ (red trace) in the presence and absence of flow and 100 nM DEA/NO. These measurements were performed in the presence of 0.2 mM EGTA. Data are shown as mean ± SEM ( n = 25 thrombi). j Traces between time points t 1 and t 2 of i are shown with inverted Ca 2+ traces to facilitate analysis of the chronological order of changes in cGMP and Ca 2+ . Results are representative of three independent experiments
Techniques Used: Activity Assay, Concentration Assay, Imaging, Expressing, Western Blot
2) Product Images from "Characterization and regulation of wild‐type and mutant TASK‐1 two pore domain potassium channels indicated in pulmonary arterial hypertension"
Article Title: Characterization and regulation of wild‐type and mutant TASK‐1 two pore domain potassium channels indicated in pulmonary arterial hypertension
Journal: The Journal of Physiology
Figure Legend Snippet: Effect of Riociguat (10 μm) on WT TASK‐1 and TASK‐1 variants A , plot of current (pA pF –1 ) measured at –40 mV from individual cells transiently expressing WT TASK‐1 either incubated in extracellular solution minus riociguat (control: black dots) or incubated in extracellular solution containing 10 μ m riociguat (blue squares). Error bars represent the 95% CI. B , representative currents recorded through WT TASK‐1, evoked by ramp changes in voltage from –120 mV to –40 mV under control conditions (2.5 m m [K + ] o ), (black line) and after incubation in 10 μ m riociguat (blue line). C and D , as shown for ( A ) and ( B ), but for TASK‐1_G106R channels. E and F , as shown for ( A ) and ( B ), but for TASK‐1_L214R channels. [Color figure can be viewed at wileyonlinelibrary.com ]
Techniques Used: Expressing, Incubation
3) Product Images from "Modulation of soluble guanylate cyclase ameliorates pulmonary hypertension in a rat model of chronic thromboembolic pulmonary hypertension by stimulating angiogenesis). Modulation of soluble guanylate cyclase ameliorates pulmonary hypertension in a rat model of chronic thromboembolic pulmonary hypertension by stimulating angiogenesis"
Article Title: Modulation of soluble guanylate cyclase ameliorates pulmonary hypertension in a rat model of chronic thromboembolic pulmonary hypertension by stimulating angiogenesis). Modulation of soluble guanylate cyclase ameliorates pulmonary hypertension in a rat model of chronic thromboembolic pulmonary hypertension by stimulating angiogenesis
Journal: Physiological Reports
Figure Legend Snippet: Post‐mortem computerized tomographic measurement of pulmonary vascular volumes with representative images (a = Sham, b = PE, c = PE+SU5416, d = PE+SU5416+CINA; no image available for PE+SU+RIO). CINA, cinaciguat; PE, pulmonary embolism with microspheres alone; RIO, riociguat. The asterisk indicates significance at p
Figure Legend Snippet: Geltrex tube assays of rat endothelial cells treated with SU5416 plus cinaciguat (CINA) or riociguat (RIO). Panel a: Phase‐contrast images of representative wells from triplicate assays of pulmonary microvascular endothelial cells (PMVECs) (25k/well) treated with the indicated supplements. Control cells were incubated with M1266 basal medium containing glutamine and antibiotic‐antimycotic mix without growth factors or serum. DMSO was added at a concentration of 0.2% in control samples. SU5416, CINA, and RIO dissolved in DMSO were added to M1266 basal medium at the indicated concentrations. Panel b: Angiogenesis Analyzer metrics of PMVECs treated in Panel a. Representative metrics in which SU5416+CINA treatments were significantly different from SU5416 alone are shown ( p
Techniques Used: Incubation, Concentration Assay
4) Product Images from "The soluble guanylate cyclase stimulator riociguat reduces fibrogenesis and portal pressure in cirrhotic rats"
Article Title: The soluble guanylate cyclase stimulator riociguat reduces fibrogenesis and portal pressure in cirrhotic rats
Journal: Scientific Reports
Figure Legend Snippet: Riociguat reduces hepatic inflammation. RT-PCR was performed in liver tissue to screen for expression changes of inflammatory marker. ( A ) In the early BDL model expression differences were mostly non-significant, when compared to SO-VEH. Yet, in RIO treated animals mean VCAM and TNFα were decreased by 48.5% and 46.7%, respectively. ( B ) In advanced BDL animals, RIO significantly decreased TNFα and tended to reduce MCP1 expression. ( C ) Western Blotting was used to measure hepatic TNFα protein content, which significantly decreased in BDL rats receiving RIO. ( D ) Transaminases AST and ALT were measured in serum samples. RIO caused a significant decrease of AST and a trend towards lower ALT levels in rats with advanced BDL. ( E ) Hepatic immunohistochemistry stainings of CD68 positive cells were quantified to assess macrophage infiltration. In advanced BDL rats CD68 positive cell content was significantly decreased after RIO treatment. Full-length blots of the cropped lines [ q, r ] are presented in Supplementary Figure S5 . *p
Techniques Used: Reverse Transcription Polymerase Chain Reaction, Expressing, Marker, Western Blot, AST Assay, Immunohistochemistry
Figure Legend Snippet: Riociguat exerts antifibrotic activity in cholestatic and toxic models. ( A ) Hepatic chromotrope-aniline-blue (CAB) stained area was quantified to assess fibrosis. In early and in advanced BDL rats, RIO significantly reduced CAB stained area. ( B ) In CCl4 cirrhosis RIO reduced CAB area only in early but not in advanced disease. ( C ) The liver fibrosis marker hydroxyproline content was measured photometrically and corrected to liver weight. RIO reduced hepatic hydroxyproline in both, early and advanced BDL rats. ( D ) No differences regarding hepatic hydroxyproline content were notable in early or advanced CCl4 animals receiving RIO. ( E ) Cytokeratin-19 (CK19) immunohistochemistry staining of liver slides were quantified to determine bile ducts. In early BDL-RIO rats less biliary proliferation was notable. Representative liver slides are shown in panel A, B and E. *p
Techniques Used: Activity Assay, Staining, Marker, Immunohistochemistry
Figure Legend Snippet: Riociguat improves intrahepatic vasodilation and vascular dysfunction. Western blots were performed to determine intrahepatic protein concentrations of markers of vascular contraction (total moesin [t-moesin], p-moesin, myosin), vascular dilation (t-eNOS, p-eNOS) and angiogenesis (VEGFR2, PDGFβ) in rats with ( A , B ) early and ( C , D ) advanced BDL cirrhosis. Values were normalized to expression of glyceraldehyde 3-phosphate dehydrogenase (GAPDH) as housekeeping protein. ( A ) BDL significantly increased hepatic moesin phosphorylation and myosin content in rats with early BLD cirrhosis, which was counter-regulated by RIO treatment. ( B ) VEGFR2 and PDGFβ expression increased significantly in early BDL rats, whereas after RIO treatment expression of both remained low. ( C ) RIO tended to normalize moesin phosphorylation and myosin content in rats with advanced BDL. ( D ) While eNOS protein content and phosphorylation were increased by RIO therapy, VEGFR2 and PDGFβ expression remained unchanged in advanced BDL-RIO animals. ( E , F ) Representative Western blots of early [ a-h ] and advanced [ i-p ] BDL animals. Full-length blots are presented in Supplementary Figure S5 . *p
Techniques Used: Western Blot, Expressing
Figure Legend Snippet: Study design and treatment groups. Riociguat or vehicle were gavaged once daily for 2–3 weeks to rats in early and advanced stages of cholestatic (BDL) or toxic (CCl4) cirrhosis, and to respective controls. Subsequently, portal and systemic hemodynamics were assessed and the degree of liver fibrosis quantified. The PPVL model was used to study hemodynamic effects in non-cirrhotic prehepatic portal hypertension.
5) Product Images from "Riociguat prevents hyperoxia-induced lung injury and pulmonary hypertension in neonatal rats without effects on long bone growth"
Article Title: Riociguat prevents hyperoxia-induced lung injury and pulmonary hypertension in neonatal rats without effects on long bone growth
Journal: PLoS ONE
Figure Legend Snippet: Riociguat prevents hyperoxia-impaired alveolarization. ( A ) H E stained lung histology. Hyperoxia exposure in the presence of placebo decreased radial alveolar count (RAC) ( B ) and increased mean linear intercept (MLI) ( C ) as compared with normoxia. Administration of riociguat increased RAC and decreased MLI during hyperoxia. *** P
Techniques Used: Staining
Figure Legend Snippet: Riociguat reduces and alters hyperoxia-induced lung inflammation. ( A ) Immunostaining for Mac-3, a macrophage marker. ( B ) The alveolar airspace macrophage population was increased by hyperoxia exposure as compared to normoxia. Administration of riociguat decreased macrophage count during hyperoxia. *** P
Techniques Used: Immunostaining, Marker
Figure Legend Snippet: Riociguat does not affect femur growth and structure. ( A ) Bone length. ( B ) Trabecular thickness (Tb.Th). ( C ) Trabecular number (Tb.N). ( D ) Bone volume fraction (BV/TV). ( E ) Structural model index (SMI). ( F ) Representative micro-CT images. n = 5/group.
Techniques Used: Micro-CT
Figure Legend Snippet: Riociguat decreases hyperoxia-induced vascular remodeling. ( A , C ) Double immunofluorescence staining for vWF (green signal) and α-SMA (red signal) plus DAPI nuclear stain (blue signal). ( B ) Hyperoxia exposure in the presence of placebo increased muscularization of peripheral pulmonary vessels (
Techniques Used: Double Immunofluorescence Staining, Staining
Figure Legend Snippet: Riociguat increases lung tissue cGMP levels. Riociguat significantly increased cGMP concentration in hyperoxia-exposed rats as compared with placebo treated hyperoxic rats. * P
Techniques Used: Concentration Assay
Figure Legend Snippet: Riociguat prevents hyperoxia-ablated vascular development. ( A ) Immunofluorescence staining for von-Willebrand factor (vWF) (green signal). Vascular density (VD) was determined by counting vWF-positive vessels (
Techniques Used: Immunofluorescence, Staining
Figure Legend Snippet: Riociguat reduces hyperoxia-induced PH. ( A ) Right ventricular systolic pressure (RVSP) was significantly increased in the hyperoxia + placebo treated group as compared with normoxia group. Riociguat administration significantly decreased RVSP during hyperoxia. *** P
6) Product Images from "Riociguat versus sildenafil on hypoxic pulmonary vasoconstriction and ventilation/perfusion matching"
Article Title: Riociguat versus sildenafil on hypoxic pulmonary vasoconstriction and ventilation/perfusion matching
Journal: PLoS ONE
Figure Legend Snippet: Oxygen selectivity of the vasodilator effects in isolated human arteries. Riociguat (A) and sildenafil (B) relax human pulmonary arteries (PA) bubbled with 21% O 2 -5% CO 2 -74% N 2 , 95% O 2 -5% CO 2 or with 95% N 2 -5% CO 2 (hypoxia). Arteries were initially stimulated with a cocktail of U46619 (30 nM), 5-HT (3 μM) and endothelin (3 nM) and, thereafter, the drugs were added in a cumulative fashion (all from 10 -9 M to 10 -5 M). Results are means ± SEM (n = 11 and 10 for riociguat and 7 and 6 for sildenafil). The parameters calculated from these curves and their statistical analysis are shown in Table 1 .
Techniques Used: Isolation
Figure Legend Snippet: Effects of riociguat on ventilation-perfusion coupling (V’/Q’). Effects of riociguat on (A) ventilation (V’), (B) perfusion (Q’) and (C) ventilation-perfusion coupling (V’/Q’) in control and bleomycin-induced fibrotic rats. (D) Representative images of ventilation and perfusion were obtained by micro-CT-SPECT. A single dose of riociguat (0.1 mg/kg) or vehicle was administered 21 days after the administration or bleomycin or saline. The relationship between the ventilation and perfusion data was determined using PMOD™ software to analyze the intensity of radiation (arbitrary units) of each volume of interest. Results are means ± SEM (n = 8). *P
Techniques Used: Micro-CT, Single Photon Emission Computed Tomography, Software
Figure Legend Snippet: Riociguat and sildenafil inhibit hypoxic pulmonary vasoconstriction and U46619-induced vasoconstriction in isolated rat pulmonary arteries (PA). PA bubbled with 21% O 2 , 74% N 2 and 5% CO 2 were initially exposed to hypoxia (95% N 2 and 5% CO 2 ), then treated with the drugs (both at 100 nM), exposed again to hypoxia and finally treated with U46619 (100 nM). Panel A shows the study protocol and representative traces. Panels B and C show the results (means ± SEM, n = 12, 9 and 8 for vehicle, riociguat and sildenafil, respectively) for the effects of hypoxia and U46619, respectively. *P
Techniques Used: Isolation
Figure Legend Snippet: Oxygen and pulmonary selectivity of the vasodilator effects in isolated rat arteries. The sGC stimulators riociguat (A) and BAY412272 (B) and the PDE5 inhibitors sildenafil (C) and tadalafil (D) relax rat pulmonary (PA) and mesenteric arteries (MA) bubbled with 21% O 2 -74% N 2 -5% CO 2 , 95% O 2 -5% CO 2 or with 95% N 2 -5% CO 2 (hypoxia). Arteries were initially stimulated with a cocktail of U46619 (30 nM), 5-HT (3 μM) and endothelin (3 nM) and, thereafter, the drugs were added in a cumulative fashion (all from 10 -9 M to 10 -5 M). The insets show the correlation between the initial response to ACh (1 μM) and the subsequent relaxation induced by riociguat (0.1 μM) or sildenafil (1 μM) in each artery (data from MA and PA under all conditions). Results are means ± SEM (n = 7, 6, 6 and 6 for riociguat 7, 9, 9 and 5 for sildenafil, in PA at 21, 95, and 0% O 2 or MA, respectively, and 4, 4 and 4 for tadalafil and 6, 5 and 5 for BAY412272 in PA at 95, and 0% O 2 or MA, respectively). The parameters calculated from these curves and their statistical analysis are shown in Table 1 .
Techniques Used: Isolation
Figure Legend Snippet: Effects of riociguat and sildenafil on systemic and pulmonary arterial pressure (SAP and PAP) and oxygen arterial saturation (SpO 2 ). After stabilization, rats were ventilated with FIO 2 = 0.1 (Hyp), then vehicle, riociguat (0.1 mg/kg) or sildenafil (0.5 mg/kg) were injected IV and after 20 min again ventilated with FIO 2 = 0.1 and finally U46619 (0.003 mg/kg, U4) was injected IV. (A) Heart rate (HR), (B) SpO 2 , (C) SAP and (D) PAP. Results are means ± SEM (n = 6 for vehicle and 5 for riociguat and sildenafil). The graphs show absolute values. Relative changes and the statistical analysis of these results are shown in Fig 5 .
Techniques Used: Injection