BAY 41-2272 |
| Catalog No.GC10192 |
Activator of soluble guanylyl cyclase (sGC)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 256376-24-6
Sample solution is provided at 25 µL, 10mM.
;)
_1-7.$$$37316672@70.jpg');)
;)
;)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
;)
;)
;)
_1124-1138.$$$35908550@30.jpg');)
_766-780.$$$37100057@30.jpg');)
_418-432.$$$36893736@30.jpg');)
_240-255.$$$35108512@29.jpg');)
_533-545.$$$36543525@28.jpg');)
_264-276.$$$36600053@22.jpg');)
_2214998.$$$@0.jpg');)
BAY 41-2272 is an activator of nitric oxide-sensitive guanylyl cyclase (NO-sensitive GC) with EC50 values of 0.3 μmol/L and 3 μmol/L in the presence and absence of 100 nmol/L DEA-NO, respectively [1].
NO-sensitive GC catalyzes the cGMP formation. It is generally considered as the most important receptor of the signaling molecule NO. The NO/cGMP pathway plays a role in many physiological processes such as the inhibition of platelet aggregation and the relaxation of smooth muscle [1].
In platelets, GSNO at 3 μmol/L (a submaximally effective concentration) was used to assess a possible sensitizing effect of BAY 41-2272 on NO-sensitive GC. The cGMP response resulted from the application of NO at this concentration in the absence of BAY 41-2272 was only marginal. In the presence of BAY 41-2272 at 100 μmol/L, treatment with GSNO at 3 μmol/L resulted in a rapid increase in cGMP up to 1000 pmol/109 platelets [1].
The sGC/NO system was implicated in the pathogenesis of erectile dysfunction. Intravenous treatment with BAY 41-2272 at 1 mg/kg induced only a very weak erection in rabbits, with a maximal length of exposed mucosa of about 3mm at 10 min, and the effect lasted for approximate 30 minutes. SNP is a NO donor. Simultaneous administration of SNP potentiated the effect of BAY 41-2272. Intravenous treatment with SNP at 0.2 mg/kg resulted in a short-lasting erection of about 5~10 minutes, and a peak length of uncovered penile mucosa of 5 mm. Administration with BAY 41-2272 at 1 mg/kg IV followed by SNP at 0.2 mg/kg IV 5 minutes later, resulted in lengths of ensuing erection with a mean of 15 mm, longer than lengths resulted from treatments with two compounds separately [2].
References:
[1]. Mullershausen F, Russwurm M, Friebe A, et al. Inhibition of phosphodiesterase type 5 by the activator of nitric oxide-sensitive guanylyl cyclase BAY 41-2272. Circulation, 2004, 109(14): 1711-1713.
[2]. Bischoff E, Schramm M, Straub A, et al. BAY 41-2272: a stimulator of soluble guanylyl cyclase induces nitric oxide-dependent penile erection in vivo. Urology, 2003, 61(2): 464-467.
| Cas No. | 256376-24-6 | SDF | |
| Chemical Name | 5-cyclopropyl-2-(1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)pyrimidin-4-amine | ||
| Canonical SMILES | FC1=CC=CC=C1CN2N=C(C3=CC=CN=C23)C(N=C4N)=NC=C4C5CC5 | ||
| Formula | C20H17FN6 | M.Wt | 360.39 |
| Solubility | DMF: 16.6 mg/ml,DMF:PBS(pH 7.2)(1:6): 0.14 mg/ml,DMSO: 12.5 mg/ml,Ethanol: 0.16 mg/ml | 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. |
||
| 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 | 2.7748 mL | 13.8739 mL | 27.7477 mL |
| 5 mM | 0.555 mL | 2.7748 mL | 5.5495 mL |
| 10 mM | 0.2775 mL | 1.3874 mL | 2.7748 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *