SGC stimulator 1
sGC stimulator 1 is a carbonyl sulfide (COS)/H2S-donor hybrid soluble guanylyl cyclase (sGC) stimulator (EC50 = 496 nM). sGC stimulator 1 exhibits a well-characterized H2S-releasing property. sGC stimulator 1 reduces fibrosis in TGF-β1-treated cardiac fibroblasts by increasing cGMP and H2S levels. sGC stimulator 1 can exert anti-fibrotic effects by activating sGC and increasing H2S. sGC stimulator 1 can be used for the study of heart failure (HF).
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- Formule: C21H18F2N4O3S2
- Masse moléculaire:476.52
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
sGC stimulator 1 (25 μM) exhibits an H2S release efficiency as high as 87%[1].
sGC stimulator 1 (0-100 μM, 48 h) shows good cytocompatibility and no obvious cytotoxicity within a proper range of concentrations in cardiac fibroblasts (CFs) isolated from neonatal rats[1].
sGC stimulator 1 (50 μM, 12 h) enhances green fluorescence, indicating that sGC stimulator 1 effectively stimulates H2S production and consequently increases the H2S levels within the cellular microenvironment in CFs[1].
sGC stimulator 1 (5-20 μM) can significantly increase intracellular cGMP levels at concentrations ≥10 μM in CFs[1].
sGC stimulator 1 (2.5-10 μM, 48 h) effectively inhibits TGFβ1-induced increases in both α-SMA expression and FN-mediated ECM synthesis in CFs, indicating its synergistic effect in suppressing CF activation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Cardiac fibroblasts isolated from neonatal rats.
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Concentration:0 μM, 12.5 μM, 25 μM, 50 μM, 100 μM
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Incubation Time:48 h
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Result:Indicated good cytocompatibility.
Showed no obvious cytotoxicity within a proper range of concentrations in CFs isolated from neonatal rats.
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Cell Line:Cardiac fibroblasts isolated from neonatal rats.
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Concentration:0 μM, 2.5 μM, 5 μM, 10 μM
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Incubation Time:48 h
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Result:Effectively inhibited TGFβ1-induced α-SMA and FN expression in CFs.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | AUC0-∞ | CL | Vss |
|---|---|---|---|---|---|---|---|---|---|
| Rat | 3 mg/kg | i.p. | 2.6 h | 0.5 h | 1731.1 ng/mL | 3029 ng·h/mL | 3033.3 ng·h/mL | 0.99 L/h/kg | 3.7 L/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Isoproterenol was subcutaneously injected at a dose of 5 mg/kg/day for 3 weeks to Male C57BL/6J mice aged 8 to 10 weeks to establish myocardial fibrosis in mice[1].
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Dosage:3 mg/kg, 5 mg/kg
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Administration:Once daily, i.p.
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Result:Enhanced EF and FS in a dose-dependent manner, while reducing the enddiastolic and end-systolic volumes as well as end-diastolic and end-systolic inner diameters, indicating a pronounced therapeutic efficacy on cardiac remodeling.
Significantly reduced the ratios of ventricular weight to body weight and ventricular weight to tibia length.
Significantly increased the plasma H2S concentration in a dose-dependent manner, 17.24 μM in the low-dose group (3.0 mg/kg/day) and 39.39 μM in the high-dose group (10 mg/kg/day).
Chemical Information
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Masse moléculaire 476.52
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Formule C21H18F2N4O3S2
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SMILES
O=C(C1=C(N=C2N1C=C(C=C2OCC3=C(C=CC=C3F)F)C)C)N[C@H](C(SS4)=NC4=O)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SGC stimulator 1 Related Classifications
HY-178191 Related Classifications
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