2. GPCR/G Protein Neuronal Signaling MAPK/ERK Pathway PI3K/Akt/mTOR
  3. mAChR p38 MAPK Akt
  4. Darifenacin

Darifenacin (UK-88525) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin inhibits tumor growth in colorectal cancer cells and has anti-tumor effects.

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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Customer Review

Based on 7 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.

    View All mAChR Isoform Specific Products:

    View All Isoforms
    mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

    View All p38 MAPK Isoform Specific Products:

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    p38 MAPK p38α p38β MAPK13 p38δ p38γ

    View All Akt Isoform Specific Products:

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    Akt Akt1 Akt2 Akt3

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Darifenacin (UK-88525) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin inhibits tumor growth in colorectal cancer cells and has anti-tumor effects[1][2][3][4][5][6].

    IC50 & Target[3]

    mAChR3

     

    ERK1

     

    ERK2

     

    MMP-1

     

    Cellular Effect
    Cell Line Type Value Description References
    CHO EC50
    > 10 μM
    Compound: 1
    Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase in GTPgamma35S binding by scintillation proximity assay
    Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase in GTPgamma35S binding by scintillation proximity assay
    		[PMID: 22932315]
    HEK293 EC50
    0.82 nM
    Compound: 4
    Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
    Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
    		[PMID: 21310610]
    HEK293 EC50
    11 nM
    Compound: 2
    Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition a
    Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition a
    		[PMID: 32202101]
    HEK293 EC50
    32 nM
    Compound: 2
    Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
    Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
    		[PMID: 32202101]
    HEK293 EC50
    45 nM
    Compound: 2
    Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
    Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
    		[PMID: 32202101]
    In Vitro

    Darifenacin (0.01-100 μM; 5 min) inhibits the Kv currents in concentration-dependent manners with an IC50 value of 0.34 μM and a Hill coefficient of 0.84 in coronary arterial smooth muscle cells[2].
    Darifenacin (0.01-10 μM; 1-48 h) inhibits cell viability, invasion and MMP-1 expression in colorectal cancer cells, and inhibits the phosphorylation of p38, ERK1/2 and Akt induced by muscarinic acetylcholine [3].

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

    Darifenacin Related Antibodies

    Cell Viability Assay[3]

    Cell Line: HT-29 and SW480 cells
    Concentration: 0.01, 0.1, 1 and 10 μM
    Incubation Time: 48 h
    Result: Reduced viability and proliferation at a concentration of 10 µM in both cell lines HT29 and SW480.

    Western Blot Analysis[3]

    Cell Line: HT-29 cells
    Concentration: 0.1, 1 and 10 μM
    Incubation Time: 1 h
    Result: Inhibited the phosphorylation levels of p38, ERK1/2 and Akt.
    In Vivo

    Darifenacin (2.5 mg/kg; Intraperitoneal injection; 42 days) has an antitumor effect in a xenograft mouse model of colorectal cancer[3].
    Darifenacin (0.1 mg/kg; Intravenous injection; Single dose) decreases the afferent activity of bladder Aδ and C fibers in female rats[4].
    Darifenacin (3 mg/kg/day; Subcutaneous osmotic pump; 14 weeks) increases the severity of liver damage caused by Azoxymethane (HY-111375)[5].

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

    Animal Model: HT-29 cells treated male BALB/cnu/nu nude mice aged 6-10 weeks old (20-25 g)[3]
    Dosage: 2.5 mg/kg
    Administration: Intraperitoneal injection (i.p.); 42 days
    Result: Reduced primary tumor volume and weight, as well as liver metastases.
    Had no significant effect on the weight of mice.
    Animal Model: Azoxymethane (HY-111375) treated male mice [genetic background: 129S6/SvEv X CF1 (50%:50%)][5]
    Dosage: 3 mg/kg/day
    Administration: Subcutaneous osmotic pump; 14 weeks
    Result: Caused the mice weigh less, reduced liver-weight-to-body-weight ratios.
    Increased liver nodularity and Ishak fibrosis scores.
    Increased in ductular proliferation.
    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; Need ultrasonic; 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.

    • Molarity Calculator

    • Dilution Calculator

    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:

    Dosage

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    (per animal)

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    Dosing volume
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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    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

    Purity: 99.81%

    SDS (252 KB)

    COA (249 KB) HNMR (277 KB) LCMS (90 KB)

    Handling Instructions (2659 KB)
    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 88525mAChRp38 MAPKAktMuscarinic acetylcholine receptorPKBProtein kinase BLiver damage modelColorectal cancer modelHT-29 cellsSW480 cellsCoronary arterial smooth muscle cellsM3 Muscarinic Receptor AntagonistInhibitorinhibitorinhibit

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