product name BAY 41-2272
Description: 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. 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.
References: Circulation. 2004 Apr 13;109(14):1711-3; Nature. 2001 Mar 8;410(6825):212-5; J Urol. 2003 Feb;169(2):761-6.
360.39
Formula
C20H17FN6
CAS No.
256376-24-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 35 mg/mL (97.1 mM)
Water: <1 mg/mL
Ethanol: 4 mg/mL (11.09 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: In vitro, BAY 41-2272 results in concentration dependent relaxation of human and rabbit cavernosum with EC50 of 489.1 nM and 406.3 nM, respectively. Kinase Assay: 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. Cell Assay: 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. |
|---|---|
| In Vivo | In female spontaneously hypertensive rats, BAY 41-2272 (10 mg/kg, p.o.) shows antiplatelet effect, strongly decreases blood pressure and increases survival. In C. albicans-infected mice, BAY 41-2272 (10 mg/kg, i.p.) markedly increases macrophage-dependent cell influx to the peritoneum in addition to macrophage functions, and reduces the death rate. In db/db-/- type II diabetic and obese mice, BAY 41-2272 improves impaired corpus cavernosum (CC) relaxation. |
| Animal model | Female spontaneously hypertensive rats |
| Formulation & Dosage | Dissolved in 10/20/70 (v/v/v) Transcutol/Cremophor EL/water; 1 mg/kg; p.o. |
| References | Circulation. 2004 Apr 13;109(14):1711-3; Nature. 2001 Mar 8;410(6825):212-5; J Urol. 2003 Feb;169(2):761-6. |
