| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
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| Targets |
Soluble guanylate cyclase (sGC)[1]
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|---|---|
| ln Vitro |
Combining WS with BAY-747 (100 nM) improves AMPA receptor kinetics in an in vitro harvest-like cLTP model [1].
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| ln Vivo |
During the study period, BAY-747 showed a brain-to-plasma ratio of 0.6 ± 2.0, indicating a comparatively high brain penetration of 60%[1]. Short-term memory impairment caused by L-NAME is lessened by BAY-747 (0.03-1.0 mg/kg, 2 mL/kg; oral; 30 min before T1 in 24-hour OLT), which improves long-term memory acquisition. The hippocampal GluA1-containing AMPAR dynamics are unaffected by BAY-747[1]. In rats receiving the l-NAME Body weight transgenic model, BAY-747 (0.003-0.3 mg/kg; oral; single dose) lowers blood pressure and (3 mg/kg; oral; once day for 35 days) raises renin[2]. In male mdx/mTRG2 mice, BAY-747 (150 mg/kg chow; oral; 16 weeks) improves skeletal muscle function by increasing grip strength and running speed[3].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: ex vivo acquisition-like cLTP model Tested Concentrations: 100 nM Incubation Duration: Experimental Results: Increased the phosphorylation levels of S845 on GluA1. |
| Animal Protocol |
Animal/Disease Models: Rat object location task (OLT) model[1]
Doses: 0.01 mg/kg, 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg Route of Administration: PO; 30 min before T1 in a 24 h interval OLT Experimental Results: Resulted Dramatically higher long-term memory performance at 0.03, 0.1, 0.3 and 1.0 mg/kg dose, 30 min before T1. Attenuated L-NAME induced short-term memory impairments at 0.3 mg /kg and 1 mg/kg. Did not enhance GluA1 trafficking at 1 mg/kg 24 h after treatment. Animal/Disease Models: Anesthetized, conscious spontaneously hypertensive and conscious normotensive rats[2] Doses: 0 mg/kg, 0.003 mg/kg, 0.01 mg/kg, 0.03 mg/kg, 0.1 mg/kg, and 0.3 mg/kg Route of Administration: IV; single dose Experimental Results: Produced a dose-dependent and long-lasting decrease in blood pressure in rats. Animal/Disease Models: l-NAME -Treated Renin Transgenic Rats[2] Doses: 0.3 mg/kg, 3 mg/kg Route of Administration: PO; one time/day for 35 days; l-NAME treatment: 30 mg/kg, po, for 6 days Experimental Results: Resulted a significant weight gain among rats. Led to a dose-depend |
| References |
[1]. Nelissen E, et al. The sGC stimulator BAY-747 and activator runcaciguat can enhance memory in vivo via differential hippocampal plasticity mechanisms. Sci Rep. 2022 Mar 4;12(1):3589.
[2]. Vakalopoulos A, et al. New Generation of sGC Stimulators: Discovery of Imidazo[1,2-a]pyridine Carboxamide BAY 1165747 (BAY-747), a Long-Acting Soluble Guanylate Cyclase Stimulator for the Treatment of Resistant Hypertension. J Med Chem. 2023 Apr 11. [3]. Krishnan SM, et al. Assessing the Use of the sGC Stimulator BAY-747, as a Potential Treatment for Duchenne Muscular Dystrophy. Int J Mol Sci. 2021 Jul 27;22(15):8016. |
| Molecular Formula |
C22H26F2N4O2
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|---|---|
| Molecular Weight |
416.46
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| CAS # |
1609342-18-8
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| 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4012 mL | 12.0060 mL | 24.0119 mL | |
| 5 mM | 0.4802 mL | 2.4012 mL | 4.8024 mL | |
| 10 mM | 0.2401 mL | 1.2006 mL | 2.4012 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.
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