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Avanafil
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Avanafil图片
CAS NO:330784-47-9
规格:≥98%
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议
1g电议
2g电议
5g电议
10g电议

产品介绍
理化性质和储存条件
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[C@H](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

实验参考方法
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.