| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
BAY-41-8543 targets soluble guanylate cyclase (sGC), a key enzyme in the nitric oxide (NO) signaling pathway. sGC catalyzes the conversion of GTP to cyclic GMP (cGMP), a second messenger that mediates vasodilation, platelet aggregation inhibition, and other effects. BAY-41-8543 is a NO-independent stimulator of sGC that directly activates the enzyme. By stimulating sGC, it increases cGMP production, leading to vasodilation and other beneficial effects.
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| ln Vitro |
In vitro, BAY-41-8543 is a potent stimulator of sGC activity. It increases the activity of recombinant sGC in a dose-dependent manner, from 0.1 nM to 100 μM, up to 92-fold. It also inhibits collagen-induced platelet aggregation. These in vitro studies confirm BAY-41-8543's mechanism of action as a potent sGC stimulator with antiplatelet activity.
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| ln Vivo |
BAY 41-8543 (10-100 μg/kg; IV) increases cardiac output, produces dose-dependent reductions in systemic arterial pressure, and causes smaller drops in pulmonary arterial pressure[1].
(0.003, 0.01, 0.03, 0.1, and 0.3 mg/kg; iv) causes a dose-dependent and sustained drop in blood pressure in anaesthetized rats. Beyond the 30-minute observation period, BAY 41-8543 continues to lower blood pressure. BAY 41-8543 (0.1, 0.3, and 1.0 mg kg; oral) has the highest potential to lower blood pressure. The maximum dosages of BAY41-8543 have blood pressure-lowering effects that last longer than the 120-minute observation period[2].
BAY 41-8543 (3 mg/kg; p.o.; twice daily; for 5 weeks) totally blocks the development of the rise in systolic blood pressure in 18-week-old renin transgenic rats (TGR(mRen2)27) on L-NAME treatment. BAY 41-8543 significantly raises survival[2].
In vivo, BAY-41-8543 has been shown to reduce pulmonary vascular resistance and protect right ventricular (RV) function. It has vasodilatory activity in the pulmonary and systemic vascular beds. It also promotes lipid uptake into brown adipose tissue and increases energy expenditure in mice. These findings suggest potential therapeutic applications in cardiovascular diseases and metabolic disorders. |
| Enzyme Assay |
In vitro enzyme assays for BAY-41-8543 measure its stimulation of soluble guanylate cyclase (sGC) activity. sGC enzyme is incubated with GTP and varying concentrations of the compound. The production of cGMP is measured using a radioimmunoassay or an ELISA. The EC50 is determined from the dose-response curve. The compound's ability to stimulate sGC activity in a dose-dependent manner is confirmed.
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| Cell Assay |
In vitro cell-based assays for BAY-41-8543 are used to study its effects on cGMP signaling and platelet function. Cells expressing sGC are treated with the compound, and the levels of cGMP are measured. Platelet aggregation assays are performed to assess the compound's antiplatelet activity. The compound's ability to inhibit collagen-induced platelet aggregation is assessed. These assays confirm the compound's cellular activity as an sGC stimulator.
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| Animal Protocol |
Adult male Sprague-Dawley rats weighing 325-450 g
10, 30, and 100 μg/kg IV In vivo animal experiments for BAY-41-8543 have been conducted in animal models of cardiovascular disease. In a typical study, the compound is administered to animals, and hemodynamic parameters are measured. The compound's ability to reduce vascular resistance and improve cardiac function is assessed. Studies have also been conducted in models of metabolism to assess its effects on energy expenditure. |
| ADME/Pharmacokinetics |
BAY-41-8543 has a CAS number of 256498-66-5. It is a solid compound. For storage, it is recommended to keep the powder at -20°C. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have been characterized. BAY-41-8543 is a research compound and is not intended for human use.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for BAY-41-8543 is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. BAY-41-8543 is an sGC stimulator, and its toxicity would be related to its effects on cGMP signaling in normal tissues. As with all research chemicals, standard laboratory safety precautions should be followed.
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| References |
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| Additional Infomation |
BAY-41-8543 is a pyrazolopyridine.
BAY-41-8543 is a research compound and is not approved for any clinical or therapeutic use. It is a novel and potent NO-independent stimulator of soluble guanylate cyclase (sGC). BAY-41-8543 increases sGC activity in a dose-dependent manner, leading to vasodilation and antiplatelet effects. It has been investigated for the treatment of cardiovascular diseases. BAY-41-8543 is a valuable research tool for studying the sGC/cGMP signaling pathway. |
| Molecular Formula |
C21H21FN8O
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|---|---|
| Molecular Weight |
420.44
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| Exact Mass |
420.182
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| Elemental Analysis |
C, 59.99; H, 5.03; F, 4.52; N, 26.65; O, 3.81
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| CAS # |
256498-66-5
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| Related CAS # |
256498-66-5
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| PubChem CID |
9953906
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
599.7±50.0 °C at 760 mmHg
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| Flash Point |
316.5±30.1 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.762
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| LogP |
-1.16
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
584
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1=C(C=CC=C1)CN2N=C(C3=CC=CN=C32)C4=NC(N)=C(C(N)=N4)N5CCOCC5
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| InChi Key |
AQYFUZRYBJBAGZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H21FN8O/c22-15-6-2-1-4-13(15)12-30-21-14(5-3-7-25-21)16(28-30)20-26-18(23)17(19(24)27-20)29-8-10-31-11-9-29/h1-7H,8-12H2,(H4,23,24,26,27)
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| Chemical Name |
2-[1-[(2-fluorophenyl)methyl]pyrazolo[3,4-b]pyridin-3-yl]-5-morpholin-4-ylpyrimidine-4,6-diamine
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| Synonyms |
BAY-41-8543; BAY418543; BAY41-8543; UNII-323T2C09SG
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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) |
DMF: ~16.7 mg/mL (~39.7 mM)
Ethanol: ~1 mg/mL (2.4 mM) DMSO: < 1 mg/mL |
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3785 mL | 11.8923 mL | 23.7846 mL | |
| 5 mM | 0.4757 mL | 2.3785 mL | 4.7569 mL | |
| 10 mM | 0.2378 mL | 1.1892 mL | 2.3785 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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