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

Darifenacin hydrobromide (Synonyms: UK-88525 (hydrobromide))

Cat. No.: HY-A0012 Purity: 95.14%
Handling Instructions

Darifenacin hydrobromide (UK-88525 hydrobromide) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.

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

Darifenacin hydrobromide Chemical Structure

Darifenacin hydrobromide Chemical Structure

CAS No. : 133099-07-7

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10 mM * 1 mL in DMSO USD 55 In-stock
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100 mg USD 190 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Darifenacin hydrobromide:

Top Publications Citing Use of Products

    Darifenacin hydrobromide 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.
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    Description

    Darifenacin hydrobromide (UK-88525 hydrobromide) 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

    507.46

    Formula

    C₂₈H₃₁BrN₂O₂

    CAS No.

    133099-07-7

    SMILES

    O=C(C(C1=CC=CC=C1)([[email protected]@H]2CCN(CCC3=CC4=C(OCC4)C=C3)C2)C5=CC=CC=C5)N.Br

    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 : 33.33 mg/mL (65.68 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9706 mL 9.8530 mL 19.7060 mL
    5 mM 0.3941 mL 1.9706 mL 3.9412 mL
    10 mM 0.1971 mL 0.9853 mL 1.9706 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 95.14%

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    Product Name:
    Darifenacin hydrobromide
    Cat. No.:
    HY-A0012
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