2. GPCR/G Protein Autophagy PI3K/Akt/mTOR Epigenetics TGF-beta/Smad
  3. Guanylate Cyclase Autophagy AMPK TGF-β Receptor
  4. 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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SGC stimulator 1

SGC stimulator 1 Chemical Structure

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SGC stimulator 1 Related Antibodies

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Description

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)[1].

In Vitro

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.

SGC stimulator 1 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: Cardiac fibroblasts isolated from neonatal rats.
Concentration: 0 μM, 12.5 μM, 25 μM, 50 μM, 100 μM
Incubation Time: 48 h
Result: Indicated good cytocompatibility.
Showed no obvious cytotoxicity within a proper range of concentrations in CFs isolated from neonatal rats.

Western Blot Analysis[1]

Cell Line: Cardiac fibroblasts isolated from neonatal rats.
Concentration: 0 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time: 48 h
Result: Effectively inhibited TGFβ1-induced α-SMA and FN expression in CFs.
In Vivo

sGC stimulator 1 (3 mg/kg, 5 mg/kg, i.p., once daily for 3 weeks) can effectively improve cardiac systolic and diastolic function, reduce cardiac enlargement and ventricular remodeling in Isoproterenol (ISO) (HY-B1670)-induced heart failure mice, and increase plasma H2S levels in a dose-dependent manner[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].
Dosage: 3 mg/kg, 5 mg/kg
Administration: Once daily, i.p.
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).
Molecular Weight

476.52

Formula

C21H18F2N4O3S2
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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SGC stimulator 1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SGC stimulator 1SGC stimulator1SGC stimulator-1Guanylate CyclaseAutophagyAMPKTGF-β ReceptorAMP-activated protein kinaseTransforming growth factor beta receptorsHeart FailureHFSoluble Guanylyl CyclasesGCTransforming Growth Factor-Beta 1TGF-β1IsoproterenolISOInhibitorinhibitorinhibit

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