Flavoxate
Based on 1 Customer Validation
Flavoxate (Rec-7-0040 free base; DW61 free base) is an orally active L-type Ca2+ channel inhibitor and antispasmodic. Flavoxate inhibits cyclic adenosine monophosphate production by blocking voltage-dependent inward Ba2+ currents, regulating the brainstem micturition center, and stimulating G protein-coupled receptors. Consequently, Flavoxate induces relaxation of bladder smooth muscle and inhibits isovolumetric rhythmic contractions. Flavoxate effectively increases bladder capacity and alleviates symptoms of urgent urination frequency and pollakiuria caused by overactive bladder. Flavoxate can be used in research on overactive bladder and related voiding dysfunctions.
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- Reinheit: 98.07%
- CAS. Nr.: 15301-69-6
- Formel: C24H25NO4
- Molecular Weight:391.46
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
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Biologische Aktivität
Flavoxate (100 nM-30 μM) causes concentration-dependent relaxation of K+-precontracted human detrusor muscle strips, with an IC50 of 2 μM[1].
Flavoxate (10-30 μM; 5 minutes) inhibits voltage-dependent, nifedipine-sensitive Ba2+ currents (L-type Ca2+ channel currents) in freshly isolated human detrusor myocytes in a voltage- and concentration-dependent manner, with a Ki value of 10 μM at a holding potential of -60 mV and 56 μM at a holding potential of -90 mV[1].
Flavoxate (1-30 μM; 22°C, 30°C, 37°C) inhibits voltage-dependent inward Ba2+ currents through L-type Ca2+ channels in human detrusor muscle cells in a concentration-dependent and temperature-sensitive manner, with enhanced efficacy at higher temperatures (Ki=10.3 μM at 22°C, Ki=5.1 μM at 30°C, Ki=4.6 μM at 37°C), and shifts the steady-state inactivation curve leftward at 30°C[2].
Flavoxate (10-8-10-5 M; 15 min) concentration-dependently inhibits cAMP production in membrane preparations from rat striatum and cerebral cortex via pertussis toxin-sensitive G1-coupled receptors; its inhibitory effect at 10-6 M is completely reversed by combined treatment with any two of adenosine A1, dopamine D2, or adrenergic α2 receptor antagonists[3].
Flavoxate (10-8-10-4 M) binds to rat adenosine A1, adrenergic α2, dopamine D2, and muscarinic M2 receptors with Ki values in the micromolar to submicromolar range, but shows negligible affinity for many other neurotransmitter receptors[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 15301-69-6
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Appearance Solid
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Molecular Weight 391.46
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Formel C24H25NO4
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Color White to off-white
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SMILES
O=C(C1=C2C(C(C(C)=C(C3=CC=CC=C3)O2)=O)=CC=C1)OCCN4CCCCC4
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Synonyms
Rec-7-0040 free base; DW61 free base
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 20 mg/mL (51.09 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (5.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Tomoda T, et al. The effects of flavoxate hydrochloride on voltage-dependent L-type Ca2+ currents in human urinary bladder. Br J Pharmacol. 2005;146(1):25-32. [Content Brief]
[2]. Tomoda T, et al. Effects of flavoxate hydrochloride on voltage-dependent Ba2+ currents in human detrusor myocytes at different experimental temperatures. Naunyn Schmiedebergs Arch Pharmacol. 2007;376(3):195-203. [Content Brief]
[3]. Oka M, et al. Brain pertussis toxin-sensitive G proteins are involved in the flavoxate hydrochloride-induced suppression of the micturition reflex in rats. Brain Res. 1996;727(1-2):91-98. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5545 mL | 12.7727 mL | 25.5454 mL | 63.8635 mL |
| 5 mM | 0.5109 mL | 2.5545 mL | 5.1091 mL | 12.7727 mL | |
| 10 mM | 0.2555 mL | 1.2773 mL | 2.5545 mL | 6.3863 mL | |
| 15 mM | 0.1703 mL | 0.8515 mL | 1.7030 mL | 4.2576 mL | |
| 20 mM | 0.1277 mL | 0.6386 mL | 1.2773 mL | 3.1932 mL | |
| 25 mM | 0.1022 mL | 0.5109 mL | 1.0218 mL | 2.5545 mL | |
| 30 mM | 0.0852 mL | 0.4258 mL | 0.8515 mL | 2.1288 mL | |
| 40 mM | 0.0639 mL | 0.3193 mL | 0.6386 mL | 1.5966 mL | |
| 50 mM | 0.0511 mL | 0.2555 mL | 0.5109 mL | 1.2773 mL |
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