| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Soluble guanylate cyclase (sGC)[1]
Soluble guanylate cyclase (sGC). BAY-747 is a stimulator of sGC, the primary receptor for nitric oxide (NO). Activation of sGC increases cGMP production, leading to vasodilation and blood pressure reduction, as well as other downstream effects. |
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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].
BAY-747 is a highly potent sGC stimulator in cell-free enzyme assays. The imidazo[1,2-a]pyridine carboxamide class of compounds, to which BAY-747 belongs, exhibits excellent potency and selectivity for sGC, leading to sustained cGMP elevation and vasodilation in vitro. |
| 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].
In spontaneously hypertensive (SH) rats, BAY-747 causes a dose-related and long-lasting decrease in mean arterial blood pressure (MAP). It also reverses L-NAME-induced memory deficits and enhances cognition in the object location task (OLT) in rats, showing both cardiovascular and cognitive benefits. |
| Enzyme Assay |
A cell-free sGC enzyme activity assay is performed using purified recombinant human sGC. The enzyme is incubated in a reaction buffer containing GTP and varying concentrations of BAY-747. The amount of cGMP produced is quantified by a luminescence-based method or competitive ELISA to calculate the EC50 for sGC stimulation, demonstrating its potent activity.
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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. A functional cellular assay can be performed in rat aortic smooth muscle cells. Cells are treated with varying concentrations of BAY-747. sGC activity is measured by quantifying intracellular cGMP accumulation using an ELISA kit. This assay confirms that BAY-747 is a potent activator of sGC in its native cellular environment. |
| 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 In vivo efficacy is evaluated in L-NAME-treated rat models of cognitive impairment. BAY-747 is administered orally. Cognition is assessed using the object location task (OLT). For hypertension studies, spontaneously hypertensive rats are treated orally with BAY-747, and mean arterial blood pressure is measured via telemetry or tail-cuff plethysmography. |
| ADME/Pharmacokinetics |
BAY-747 exhibits an excellent pharmacokinetic profile across species, characterized by a long half-life and a low peak-to-trough ratio. Its oral bioavailability is sufficient for once-daily dosing. The compound also shows good brain penetration, with a brain-to-plasma ratio of approximately 0.6 (60%).
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| Toxicity/Toxicokinetics |
In vivo toxicology studies in rats and dogs show that BAY-747 is generally well-tolerated at therapeutic doses. High doses can cause hypotension, which is an on-target effect. The compound was investigated in resistant hypertension models, and careful dose titration is required to avoid life-threatening hypotension in combination with other antihypertensives.
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| References |
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| Additional Infomation |
BAY-747 (BAY 1165747) is a next-generation sGC stimulator from Bayer, developed as a treatment for resistant hypertension. It is structurally distinct from earlier sGC stimulators like riociguat, offering improved pharmacokinetics with a long duration of action. BAY-747 is still in preclinical and early clinical development, and its unique ability to both lower blood pressure and improve cognitive function makes it a promising candidate for conditions where both aspects are relevant, such as hypertension with associated cognitive decline.
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| CAS # |
1609342-18-8
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| Appearance |
Typically exists as solid at room temperature
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| HS Tariff Code |
2934.99.9001
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| 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)
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| 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
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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.) |
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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