ダリフェナシン
- ¥260800 - ¥579600
- 化學(xué)名: ダリフェナシン
- 英語名: Darifenacin
- 別名:ダリフェナシン;2-[(3S)-1-[2-(2,3-ジヒドロ-1-ベンゾフラン-5-イル)エチル]ピロリジン-3-イル]-2,2-ジフェニルアセトアミド;ジフェニル[(3S)-1-[2-(2,3-ジヒドロベンゾフラン-5-イル)エチル]ピロリジン-3-イル]アセトアミド;(3S)-1-[2-[(2,3-ジヒドロベンゾフラン)-5-イル]エチル]-α,α-ジフェニル-3-ピロリジンアセトアミド
- CAS番號: 133099-04-4
- 分子式: C28H30N2O2
- 分子量: 426.55
- EINECS:
- MDL Number:MFCD00896313
2物価
選択條件:
ブランド
- 富士フイルム和光純薬株式會社(wako)
パッケージ
- 250mg
- 1g
- 生産者富士フイルム和光純薬株式會社(wako)
- 製品番號W01MAS093128
- 製品説明
- 英語製品説明2-(1-(2-(2,3-Dihydrobenzofuran-5-yl)ethyl)-pyrrolidin-3-yl)-2,2-diphenylacetamide
- 包裝単位1g
- 価格¥579600
- 更新しました2024-03-01
- 購入
- 生産者富士フイルム和光純薬株式會社(wako)
- 製品番號W01MAS093128
- 製品説明
- 英語製品説明2-(1-(2-(2,3-Dihydrobenzofuran-5-yl)ethyl)-pyrrolidin-3-yl)-2,2-diphenylacetamide
- 包裝単位250mg
- 価格¥260800
- 更新しました2024-03-01
- 購入
生産者 | 製品番號 | 製品説明 | 包裝単位 | 価格 | 更新時間 | 購入 |
---|---|---|---|---|---|---|
富士フイルム和光純薬株式會社(wako) | W01MAS093128 | 2-(1-(2-(2,3-Dihydrobenzofuran-5-yl)ethyl)-pyrrolidin-3-yl)-2,2-diphenylacetamide |
1g | ¥579600 | 2024-03-01 | 購入 |
富士フイルム和光純薬株式會社(wako) | W01MAS093128 | 2-(1-(2-(2,3-Dihydrobenzofuran-5-yl)ethyl)-pyrrolidin-3-yl)-2,2-diphenylacetamide |
250mg | ¥260800 | 2024-03-01 | 購入 |
プロパティ
比旋光度 :25D -20.6° (c = 1.0 in methylene chloride)
沸點 :614.3±55.0 °C(Predicted)
比重(密度) :1.192±0.06 g/cm3(Predicted)
貯蔵溫度 :2-8°C
溶解性 :Soluble in DMSO
外見 :Powder
酸解離定數(shù)(Pka) :pKa (25°): 9.2
色 :White to off-white
沸點 :614.3±55.0 °C(Predicted)
比重(密度) :1.192±0.06 g/cm3(Predicted)
貯蔵溫度 :2-8°C
溶解性 :Soluble in DMSO
外見 :Powder
酸解離定數(shù)(Pka) :pKa (25°): 9.2
色 :White to off-white
安全情報
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説明
Darifenacin is a novel muscarinic M3 selective antagonist for the once-daily oral treatment of urinary incontinence and overactive bladder. The majority of overactive bladder symptoms are thought to result from the overactivity of the detrusor muscle, which is primarily mediated by acetylcholine-induced stimulation of muscarinic M3 receptors in the bladder. Consequently, antimuscarinic agents have become the mainstay of overactive bladder treatment. Darifenacin has a higher level of M3 selectivity than the previously marketed antimuscarinic agents. It has Ki values of 16nM for M1, 50 nM for M2, and 1.6 nM for M3 receptors. It is slightly more M3 selective than solifenacin (M1:Ki=25 nM, M2:Ki=126 nM, M3:Ki=10 nM), which was launched in 2004. Darifenacin is significantly more selective than other muscarinics such as tolterodine, oxybutynin, and trospium, which are all essentially equipotent against M1, M2, and M3 receptors. In addition,darifenacin demonstrates greater effect on tissues in which the predominant receptor type is M3 rather than M1 or M2. In vitro darifenacin inhibits carbacholinduced contractions with greater potency in isolated guinea-pig bladder (M3) than in guinea-pig atria (M2) or dog saphenous vein (M1). In animal models, it shows greater selectivity for inhibition of detrusor contraction over salivation or tachycardia.Darifenacin is supplied as a controlled release formulation, and the recommended dosage is 7.5 mg once, daily. Darifenacin is rapidly and completely absorbed from the GI tract after oral administration, with maximum plasma levels achieved after about 7 h. The elimination half-life is approximately 3 h, but because of the controlled release characteristics of the formulation, the drug is suitable for once-daily dosing. Steady-state plasma levels are achieved within 6 days of commencing treatment. Darifenacin exhibits high-protein binding (98%), a volume of distribution of 163 L, and a clearance of 40 L/h. It has low oral bioavailability (15–19%) due to extensive first-pass metabolism by CYP3A4 and CYP2D6, but this can be saturated after multiple administrations. The major circulating metabolites are produced by monohydroxylation and N-dealkylation; however, none contribute significantly to the overall clinical effect of darifenacin. Approximately 58% of the dose is excreted in urine and 44% in feces; only a small percentage (3%) of the excreted dose is unchanged darifenacin.関連商品価格
- アセトアミド
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