| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
The H2S release efficiency of sGC stimulator 1 (25 μM) was as high as 87%[1]. sGC stimulator 1 (0-100 μM, 48 h) showed good cell compatibility with neonatal rat CFs cells within an appropriate concentration range and had no obvious cytotoxicity[1]. sGC stimulator 1 (0-100 μM, 48 h) showed good cell compatibility with cardiac fibroblasts (CFs) isolated from neonatal rats and had no obvious cytotoxicity within an appropriate concentration range[1]. sGC stimulator 1 (5-20 μM) significantly increased the intracellular cGMP level in CFs cells at concentrations greater than 10 μM[1]. sGC stimulator 1 (2.5-10 μM, 48 h) effectively inhibited TGFβ1-induced α-SMA expression and FN-mediated ECM synthesis increase in CFs, indicating that it has a synergistic effect in inhibiting CF activation[1].
|
|---|---|
| ln Vivo |
sGC stimulator 1 (3 mg/kg, 5 mg/kg, intraperitoneal injection, once daily for 3 weeks) can effectively improve isoprofen (ISO)-induced cardiac stretch systolic and diastolic function, reduce cardiac enlargement and ventricular dilation, and increase myocardial H2S levels in a dose-coupled manner [1].
|
| Cell Assay |
Cell Cytotoxicity Assay[1]
Cell Types: Cardiac fibroblasts isolated from neonatal rats. Tested Concentrations: 0 μM, 12.5 μM, 25 μM, 50 μM, 100 μM Incubation Duration: 48 h Experimental Results: Indicated good cytocompatibility. Showed no obvious cytotoxicity within a proper range of concentrations in CFs isolated from neonatal rats. Western Blot Analysis[1] Cell Types: Cardiac fibroblasts isolated from neonatal rats. Tested Concentrations: 0 μM, 2.5 μM, 5 μM, 10 μM Incubation Duration: 48 h Experimental Results: Effectively inhibited TGFβ1-induced α-SMA and FN expression in CFs. |
| Animal Protocol |
Animal/Disease Models: 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].
Doses: 3 mg/kg, 5 mg/kg Route of Administration: Once daily, i.p. Experimental Results: 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). |
| References |
| Molecular Formula |
C21H18F2N4O3S2
|
|---|---|
| Molecular Weight |
476.52
|
| Appearance |
Typically exists as solids at room temperature
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0985 mL | 10.4927 mL | 20.9855 mL | |
| 5 mM | 0.4197 mL | 2.0985 mL | 4.1971 mL | |
| 10 mM | 0.2099 mL | 1.0493 mL | 2.0985 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
