Avanafil

製品コードS4019 バッチS401902

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₃H₂₆ClN₇O₃
	分子量	483.95	CAS No.	330784-47-9
Solubility (25°C)*	体外	DMSO	97 mg/mL (200.43 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Avanafil is a highly selective PDE5 inhibitor with IC50 of 5.2 nM, >121-fold selectivity over other PDEs.
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. ^[1] The cavernous injection of avanafil (1 μM) in T2DM rats results in partial improvement in erectile responses. ^[2]
特徴	Highly selective for PDE5.

プロトコル(参考用のみ)

キナーゼアッセイ	PDE Assay
キナーゼアッセイ	PDE1, 2, 3, 4, 5 and 6 activity is assayed using 1 μM cGMP, 1 μM cGMP, 1 μM cAMP, 1 μM cAMP, 1 μM cGMP and 10 μM cGMP, respectively, as the substrate. PDE7, 8, 9, 10 and 11 activity is assayed using 0.1 μM cAMP, 0.05 μM cAMP, 0.05 μM cGMP, 0.25 μM cAMP and 1 μM cGMP, respectively, as the substrate. PDE assay is done by the radiolabeled nucleotide method.7 PDE enzyme (100 μl) in 50 mM Tris-HCl (pH 8.) is added to 200 μl assay buffer composed of 50 mM Tris-HCl (pH 8.0), 12.5 mM MgCl₂, 10 mM 2-mercaptoethanol and 0.825 mg/ml bovine serum albumin. The enzyme reaction is started by adding 200 μl substrate solution containing [3H]cGMP plus unlabeled cGMP or [³H]cAMP plus unlabeled cAMP in 50 mM Tris-HCl (pH 8.0). Reaction mixtures are incubated at 37C for 30 minutes and then boiled for 1.5 minutes. Subsequently 100 μl 1 mg/ml Crotalus atrox snake venom are added and incubated at 37C for 30 minutes. The reaction is stopped by adding 500 μl methanol. Resultant solutions are applied to a Dowex (1 × 8, 200 to 400) column (volume 0.225 ml). Eluate radioactivity is measured with 5 ml aqueous scintillation cocktails. DMSO solution without the compounds served as a control. The final concentration of DMSO in the reaction mixture is 1% volume per volume.
動物実験	動物モデル	Male mongrel dogs
	投薬量	1-300 μg/kg
	投与方法	Intraduodenal treatment or i.v.

参考

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

c-FOS drives reversible basal to squamous cell carcinoma transition [ Cell Rep, 2021, 37(1):109774]	PubMed: 34610301

c-FOS drives reversible basal to squamous cell carcinoma transition [ Cell Rep, 2021, 37(1):109774]

PubMed: 34610301

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。