product name Avanafil
Description: Avanafil is a highly potent and selective PDE5 inhibitor with IC50 of 5.2 nM, and with >121-fold selectivity over other PDEs. Avanafil was approved by FDA for the treatment of erectile dysfunction on April 27, 2012 and by EMA on June 21, 2013. Avanafil acts by inhibiting a specific phosphodiesterase type 5 enzyme which is found in various body tissues, but primarily in the corpus cavernosum penis, as well as the retina.
References: J Urol. 2012 Aug;188(2):668-74; Urology. 2014 Feb;83(2):508.e7-12.
483.95
Formula
C23H26ClN7O3
CAS No.
330784-47-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 97 mg/mL (200.4 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Avanafil is highly selective toward PDE5 and against all other PDE isozymes tested. Lower selectivity against PDE1, PDE6, and PDE11 is consistent with results from randomized, placebo-controlled, phase 3 trials in which musculoskeletal and hemodynamic adverse events were reported in <2% of patients and no color vision-related abnormalities were reported with avanafil doses up to 200mg once daily ntraduodenal doses of avanafil or sildenafil (0.1 and 1 mg/kg) potentiated the AUC of nitroglycerin induced hypotension. However, the potentiating effect of avanafil at 1 mg/kg was significantly weaker than that of sildenafil (p <0.05). Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Avanafil (i.v.) potentiates penile tumescence with ED200% of 37.5 μg/kg in dogs. Furthermore, intraduodenal treatment of Avanafil potentiates pelvic nerve stimulation induced changes in intracavernous pressure and duration. The cavernous injection of avanafil (1 μM) in T2DM rats results in partial improvement in erectile responses. |
| Animal model | Male mongrel dogs |
| Formulation & Dosage | Dissolved in 0.05N HCl (intraduodenal); Saline containing 0.01N HCl (i.v.); 1-300 μg/kg; Intraduodenal treatment or i.v. administration |
| References | J Urol. 2012 Aug;188(2):668-74; Urology. 2014 Feb;83(2):508.e7-12. |
