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    Avanafil
    Avanafil

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0797
    CAS #: 330784-47-9Purity ≥98%

    Description: Avanafil (also known as TA 1790; TA1790; TA-1790; trade name: Stendra; Spedra) is a highly potent and selective PDE5 inhibitor with potential vasodilating effects. It inhibits PDE5 with an IC50 of 5.2 nM, and shows >121-fold selectivity for PDE5 over other isoforms of PDE. As of 2012, Avanafil was approved by the US FDA for the treatment of erectile dysfunction. 

    References: J Urol. 2012 Aug;188(2):668-74; Urology. 2014 Feb;83(2):508.e7-12. 

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    Molecular Weight (MW)483.95
    FormulaC23H26ClN7O3
    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
    Other info

    Chemical Name: (S)-4-[(3-Chloro-4-methoxybenzyl)amino]-2-[2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2pyrimidinylmethyl)-5-pyrimidinecarboxamide

    InChi Key: WEAJZXNPAWBCOA-INIZCTEOSA-N

    InChi Code: InChI=1S/C23H26ClN7O3/c1-34-19-6-5-15(10-18(19)24)11-27-21-17(22(33)28-13-20-25-7-3-8-26-20)12-29-23(30-21)31-9-2-4-16(31)14-32/h3,5-8,10,12,16,32H,2,4,9,11,13-14H2,1H3,(H,28,33)(H,27,29,30)/t16-/m0/s1

    SMILES Code: O=C(C1=CN=C(N2[[email protected]](CO)CCC2)N=C1NCC3=CC=C(OC)C(Cl)=C3)NCC4=NC=CC=N4

    Synonyms

    TA 1790; TA1790; Avanafil; TA-1790; trade name: Stendra; Spedra


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    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).

    In VivoAvanafil (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 modelMale mongrel dogs 
    Formulation & DosageDissolved 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. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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