| 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 |
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BAY-41-8543 is a novel and potent NO-independent guanylyl cyclase stimulator. BAY 41-8543 is a heme-dependent sGC stimulator that raises the activity of recombinant sGC in a dose-dependent manner.
| 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].
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| Animal Protocol |
Adult male Sprague-Dawley rats weighing 325-450 g
10, 30, and 100 μg/kg IV |
| References |
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| Additional Infomation |
BAY-41-8543 is a pyrazolopyridine.
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| 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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