BAY 41-8543 |
| Catalog No.GC11426 |
BAY 41-8543 est un stimulateur de la guanylyl cyclase soluble (sGC) indépendant de l'oxyde nitrique (NO) et actif par voie orale.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 256498-66-5
Sample solution is provided at 25 µL, 10mM.
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IC50: 0.09 μM human platelets
BAY 41-8543 is a soluble guanylate cyclase (sGC) stimulator.
Soluble guanylate cyclase (sGC) has been identified as the primary cellular receptor for nitric oxide (NO). NO can bind and activate a heme group in sGC, initiating the conversion of GTP to the second messenger cyclic GMP (cGMP).
In vitro: Previous study found that BAY 41-8543 could concentration-dependently stimulate the recombinant sGC up to 92-fold. Moreover, BAY 41-8543 and NO had synergistic effects over a wide range of concentrations. Similar results were shown that BAY 41-8543 stimulated the sGC directly and further made the enzyme more sensitive to its endogenous activator NO. In addition, BAY 41-8543 was found to be a potent relaxing agent of aortas, saphenous arteries, coronary arteries and veins with IC50-values in the nm range [1].
In vivo: In anaesthetized dogs, i.v. injections of BAY 41-8543 could cause a dose-dependent decrease in blood pressure and cardiac oxygen consumption as well as an increase in coronary blood flow and heart rate. In anaesthetized normotensive rats, BAY 41-8543 produced a dose-dependent and long-lasting blood pressure lowering effect. Moreover, a dose-dependent and long-lasting decrease in blood pressure was also observed in conscious spontaneously hypertensive rats with a threshold dose of 0.1 mg/kg p.o. [2].
Clinical trial: So far, no clinical study has been conducted.
References:
1. Stasch, J.P.,Alonso-Alija, C.,Apeler, H., et al. Pharmacological actions of a novel NO-independent guanylyl cyclase stimulator, BAY 41-8543: In vitro studies. British Journal of Pharmacology 135, 333-343 (2002).
2. Stasch, J.P.,Dembowsky, K.,Perzborn, E., et al. Cardiovascular actions of a novel NO-independent guanylyl cyclase stimulator, BAY 41-8543: in vivo studies. British Journal of Pharmacology 135, 344-355 (2002).
| Cas No. | 256498-66-5 | SDF | |
| Chemical Name | 2-[1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-(4-morpholinyl)-4,6-pyrimidinediamine | ||
| Canonical SMILES | FC(C=CC=C1)=C1CN2N=C(C3=NC(N)=C(N4CCOCC4)C(N)=N3)C5=C2N=CC=C5 | ||
| Formula | C21H21FN8O | M.Wt | 420.4 |
| Solubility | ≤3mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3787 mL | 11.8934 mL | 23.7869 mL |
| 5 mM | 0.4757 mL | 2.3787 mL | 4.7574 mL |
| 10 mM | 0.2379 mL | 1.1893 mL | 2.3787 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)
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