2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. Darifenacin

Darifenacin  (Synonyms: UK-88525)

Cat. No.: HY-A0033 Purity: 99.54%
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Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.

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

Darifenacin Chemical Structure

Darifenacin Chemical Structure

CAS No. : 133099-04-4

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5 mg USD 80 In-stock
10 mg USD 120 In-stock
25 mg USD 240 In-stock
50 mg USD 360 In-stock
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Based on 6 publication(s) in Google Scholar

Other Forms of Darifenacin:

Darifenacin Related Antibodies

Top Publications Citing Use of Products

    Darifenacin purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Apr 5;7(14):18085-94.  [Abstract]

    MACC1 is up-regulated by ACh through p-AMPK. A. ACh stimulates AMPK phosphorylation via M3R. B. Inhibition of AMPK activity by Dorsomorphin (8 μM) suppresses the induction of MACC1 expression by ACh. p-AMPK levels increase after ACh stimulation, and pretreatment of Darifenacin attenuates the ACh-induced increase of p-AMPK.

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    Description

    Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. IC50 value: 8.9 (pKi) [1] Target: M3 receptor in vitro: Darifenacin exerts non-parallel rightward displacement of the agonist curve and also significant depression of the maximum response (+)-cis-Dioxolane produced concentration-dependent contraction of the isolated bladder of rat [1]. Darifenacin produces a concentration dependent increase in R123 (P-gp probe) accumulation in MDCK cells. Darifenacin stimulates ATPase activity in P-gp membrane in a clear concentration dependent response manner with an estimated ED50 value of 1.6 μM. Darifenacin (100 nM) shows a significantly greater permeability for darifenacin in the basolateral to apical direction resulting in an efflux ratio in BBMEC monolayers of approximately 2.6 [2]. in vivo: Darifenacin produces dose-dependent inhibition of amplitude of volume-induced bladder contractions(VIBCAMP), producing 35% inhibition at dose of 283.3 nmol/kg and maximal inhibition of approximately 50–55% [1]. Darifenacin (0.1 mg/kg i.v.) reduces bladder afferent activity in both Aδ and C fibers in female Sprague-Dawley rats, the decrease in afferent spikes in C fibers may be more pronounced than that in Aδ fibers [3].

    Clinical Trial
    Molecular Weight

    426.55

    Formula

    C28H30N2O2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N)C(C1=CC=CC=C1)([C@H]2CN(CCC3=CC=C(OCC4)C4=C3)CC2)C5=CC=CC=C5
    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 : 100 mg/mL (234.44 mM; ultrasonic and warming and heat to 80°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 2.3444 mL 11.7220 mL 23.4439 mL
    5 mM 0.4689 mL 2.3444 mL 4.6888 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

    Concentration (start)

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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: 2.5 mg/mL (5.86 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.5 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (5.86 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.5 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    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:
    %
    DMSO +
    % 
    +
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    Tween-80 +
    %
    Saline
    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 2.3444 mL 11.7220 mL 23.4439 mL 58.6098 mL
    5 mM 0.4689 mL 2.3444 mL 4.6888 mL 11.7220 mL
    10 mM 0.2344 mL 1.1722 mL 2.3444 mL 5.8610 mL
    15 mM 0.1563 mL 0.7815 mL 1.5629 mL 3.9073 mL
    20 mM 0.1172 mL 0.5861 mL 1.1722 mL 2.9305 mL
    25 mM 0.0938 mL 0.4689 mL 0.9378 mL 2.3444 mL
    30 mM 0.0781 mL 0.3907 mL 0.7815 mL 1.9537 mL
    40 mM 0.0586 mL 0.2930 mL 0.5861 mL 1.4652 mL
    50 mM 0.0469 mL 0.2344 mL 0.4689 mL 1.1722 mL
    60 mM 0.0391 mL 0.1954 mL 0.3907 mL 0.9768 mL
    80 mM 0.0293 mL 0.1465 mL 0.2930 mL 0.7326 mL
    100 mM 0.0234 mL 0.1172 mL 0.2344 mL 0.5861 mL
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    Darifenacin 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:

    Darifenacin133099-04-4UK-88525UK88525UK 88525mAChRMuscarinic acetylcholine receptorInhibitorinhibitorinhibit

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