バルデナフィル HCL

￥15000 - ￥120000

化学名バルデナフィル HCL

英語名Vardenafil

CAS番号224785-90-4

分子式C23H32N6O4S

分子量488.6

EINECS607-088-5

MDL NumberMFCD07773094

别名

バルデナフィル HCL

バルデナフィル

1-[[3-(1,4-ジヒドロ-5-メチル-4-オキソ-7-プロピルイミダゾ[5,1-f][1,2,4]トリアジン-2-イル)-4-エトキシフェニル]スルホニル]-4-エチルピペラジン

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価格 4 物価

生産者	包装単位	価格	製品説明
富士フイルム和光純薬株式会社(wako) W01COBQA-2726	1g	￥15000	バルデナフィル HCl Vardenafil HCl
富士フイルム和光純薬株式会社(wako) W01COBQA-2726	5g	￥37500	バルデナフィル HCl Vardenafil HCl
富士フイルム和光純薬株式会社(wako) W01COBQA-2726	25g	￥120000	バルデナフィル HCl Vardenafil HCl
Sigma-Aldrich Japan V-902	1ml	￥21600	Vardenafil dihydrochloride solution<br />1.0?mg/mL in methanol (as free base), ampule of 1?mL, certified reference material

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説明

Vardenafil is a new PDE5 inhibitor launched for oral treatment of male erectile dysfunction and it has significant structural similarity with sildenafil (Viagra^?), which was the first PDE5 inhibitor introduced in 1998 for this indication. Vardenafil is synthesized in three steps starting with a cyclization reaction of 2-ethyoxybenzamidine with 2-butyramidopropionic acid and ethoxyallyl chloride to construct the imidazotriazine ring system, followed by sulfonation to the corresponding sulfonyl chloride and subsequent condensation with 1-ethylpiperazine. The potency of PDE5 inhibition by vardenafil (IC₅₀=0.7 nM) is ～10 times greater than that of sildenafil (IC₅₀=6.6 nM). Vardenafil is typically administered in single doses of 10 and 20 mg. The time to reach maximum plasma concentration is 0.75 h, which is slightly shorter than those of sildenafil (t_max=1.16 h) and tadalafil (t_max=2h), and the half-life is 4–5 h. Although it is almost completely absorbed following oral administration, the mean absolute bioavailability of a 10 mg dose is ～15%, resulting from extensive first pass metabolism. Vardenafil is metabolized in the liver primarily by CYP3A4 and is eliminated mainly in feces. In clinical studies, 10–20 mg doses of vardenafil was well tolerated and efficacious in patients with ED of various severities, including subjects with comorbidities such as diabetes mellitus or hypertension or hyperlipidemia. The side-effect profile of vardenafil is similar to that of sildenafil, with headache, flushing, dyspepsia and nasal congestion being the most common adverse events. Vardenafil has systemic vasodilatory properties, which can cause transient decrease in supine blood pressure; however, it does not appear to translate into clinical effects. The mean maximum decreases in supine systolic blood pressure following 20 and 40 mg vardenafil were 6.9 and 4.3 mmHg, respectively, when compared to placebo. However, single and multiple oral doses of vardenafil up to 40 mg produced no clinically relevant changes in the ECGs of normal male volunteers.

融点	230-235°C
比重(密度)	1.37
蒸気圧	0.001Pa at 71.34℃
闪点	9℃
貯蔵温度	Sealed in dry,Store in freezer, under -20°C
溶解性	>22.5mg/mL in DMSO
外見	Powder
酸解離定数(Pka)	9.86±0.20(Predicted)
色	White to off-white
水溶解度	7mg/L at 20℃
BCS Class	2
InChIKey	NOIHTGOGFDFCBN-UHFFFAOYSA-N
SMILES	N12C(CCC)=NC(C)=C1C(=O)N=C(C1=CC(S(N3CCN(CC)CC3)(=O)=O)=CC=C1OCC)N2
LogP	2.5 at 23℃

バルデナフィル HCL

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