| BAY 41-2272Activator of soluble guanylyl cyclase (sGC) |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.00%
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| Cas No. | 256376-24-6 | SDF | Download 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 | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
