2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  3. mAChR Calcium Channel Adrenergic Receptor Adenosine Receptor Dopamine Receptor
  4. Flavoxate

Flavoxate  (Synonyms: Rec-7-0040 free base; DW61 free base)

Cat. No.: HY-B0549 Purity: 98.07%
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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.

For research use only. We do not sell to patients.

Flavoxate

Flavoxate Chemical Structure

CAS No. : 15301-69-6

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Other Forms of Flavoxate:

Flavoxate Related Antibodies

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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α adrenergic receptor β adrenergic receptor

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Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

  • Biological Activity

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Description

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[1][2][3].

In Vitro

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.

Flavoxate Related Antibodies
In Vivo

Flavoxate (3 mg/kg; i.v.; single dose) completely abolishes isovolumetric rhythmic bladder contractions in vehicle-pretreated female Sprague-Dawley rats, an effect that is eliminated by prior intracerebroventricular Pertussis Toxin (PTX) pretreatment[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

391.46

Formula

C24H25NO4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C2C(C(C(C)=C(C3=CC=CC=C3)O2)=O)=CC=C1)OCCN4CCCCC4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5545 mL 12.7727 mL 25.5454 mL
5 mM 0.5109 mL 2.5545 mL 5.1091 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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.

  • Protocol 1

    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.
In Vivo Dissolution Calculator
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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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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Flavoxate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Flavoxate15301-69-6Rec-7-0040DW61DW 61DW-61mAChRCalcium ChannelAdrenergic ReceptorAdenosine ReceptorDopamine ReceptorMuscarinic acetylcholine receptorCa2+ channelsCa channelsBeta ReceptorP1 receptorPhosphodiesteraseantispasmodicmuscarinicanestheticoveractive bladderlower urinary tract infectionsInhibitorinhibitorinhibit

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