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

Darifenacin (Synonyms: UK-88525)

Cat. No.: HY-A0033 Purity: 97.38%
Handling Instructions

Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.

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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Top Publications Citing Use of Products

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

    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.
    • Biological Activity

    • Technical Information

    • Purity & Documentation

    • References

    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
    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vivo:
    • 1.

      Darifenacin is dissolved in distilled water[4]. Darifenacin is prepared in vehicle (PBS mixed with DMSO at 1:1)[5].

    References
    Molecular Weight

    426.55

    Formula

    C₂₈H₃₀N₂O₂

    CAS No.

    133099-04-4

    SMILES

    O=C(N)C(C1=CC=CC=C1)([[email protected]]2CN(CCC3=CC=C(OCC4)C4=C3)CC2)C5=CC=CC=C5

    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
    Darifenacin
    Cat. No.:
    HY-A0033
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    Darifenacin

    Cat. No.: HY-A0033