Flavoxate HCl

製品コードS4027 バッチS402701

印刷

化学情報

Chemical Structure Synonyms NSC-114649 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H25NO4.HCl
分子量 427.92 CAS No. 3717-88-2
Solubility (25°C)* 体外 Water 10 mg/mL (23.36 mM)
DMSO 3 mg/mL (7.01 mM)
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
30%propylene glycol 5%Tween80 65%D5W
30.0mg/ml Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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 Flavoxate (NSC-114649) is a muscarinic AChR antagonist with IC50 of 12.2 μM.
in vitro Flavoxate displaces [3H]nitrendipine on the Ca2+ channels binding sites with IC50 of 254 μM. [1] Flavoxate (>10 μM) suppresses carbachol-induced contractions in isolated rat detrusor strips with pD value of 4.55. Flavoxate (>10 μM) suppresses Ca2+-induced contractions in isolated rat detrusor strips with pIC50 value of 4.92. [2] Flavoxate (0.01 μM −10 μM) inhibits CAMP formation in a concentration-dependent manner in membranes from the rat striatum and cerebral cortex, an action which is completely abolished by pretreating the membranes with pertussis toxin (PTX). [3] Flavoxate causes a concentration-dependent reduction of the K+-induced contraction of human urinary bladder. Flavoxate inhibits the peak amplitude of voltage-dependent nifedipine-sensitive inward Ba2+ currents in a voltage- and concentration-dependent manner with Ki value of 10 μM in human detrusor myocytes. [4] Flavoxate inhibits voltage-dependent nifedipine-sensitive inward Ba2+ currents in human detrusor myocytes at both 30 degrees C (Ki = 5.1 mM) and 37 degrees C (Ki = 4.6 mM). [5]
in vivo Flavoxate (10mg/kg) suppresses both the an initial, rapidly rising phasic contraction (phase 1) and the tonic contraction (phase 2) contractions to the same extent in rats. Flavoxate (10mg/kg) abolishes the bladder contractions without causing any change in the amplitude of the contractions in rats. Flavoxate (3 mg/kg) abolishes the efferent neural activity and the associated bladder contractions for about 10 minutes without changing the baseline vesical pressure in rats. ICV-injected (50 to 200 μg/rat) or IT-injected (100 to 200 μg/rat) Flavoxate abolishes rhythmic bladder contractions during and after injection for five to 15 minutes in a dose-dependent manner in rats. [2] Flavoxate (3 mg/kg, i.v.) abolishes rhythmic bladder contractions and the maximal intervals of voiding contractions is 7.20 min. [3]

プロトコル(参考用のみ)

キナーゼアッセイ Binding assay
Incubation is generally done in 10 mL polyethylene tubes. Tritiated ligand (20 μL) and Flavoxate under evaluation (20 μL) are added before the aliquot (1-2 mL) of tissue suspension. Flavoxate is initially tested at a 1 μM concentration. In the presence of significant displacing activity, a complete competition curve is performed. Following incubation, cold buffer is added to each sample, and the contents are rapidly vacuum-filtered through filters. The filters are then rapidly washed three times with 5 mL of buffer, places in scintillation vials, and shaken with 10 mL of Filtercount scintillation mixture. Specific binding is defined as the total binding minus the binding in the presence of the displacing agent. Binding in the presence of various concentrations of Flavoxate is expressed as a percentage of the specific binding with no drug present.
動物実験 動物モデル Sprague-Dawley rats
投薬量 10 mg/kg
投与方法 Intravenous

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。

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