Darifenacin

SKU: orb1687722

Description

Darifenacin is a selective muscarinic M3 receptor antagonist used in research to investigate overactive bladder and urinary incontinence. Its anticonvulsant properties are also studied in neurological models, with applications in both in vitro binding assays and in vivo pharmacological studies.

Research Area

Neuroscience, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 133099-04-4
• MW: 426.55
• Purity: 99.78% (May vary between batches)
• Formula: C₂₈H₃₀N₂O₂
• SMILES: C(C(N)=O)([C@H]1CN(CCC=2C=C3C(=CC2)OCC3)CC1)(C4=CC=CC=C4)C5=CC=CC=C5
• Target: Akt,AChR,p38 MAPK
• Solubility: DMSO:80 mg/mL (187.55 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.74 mM)

Bioactivity

• Target IC50:
  ATPase activity (P-gp membranes:1.6 μM (ED50)
• In Vivo:
  Darifenacin dose-dependently inhibited volume-induced bladder contraction amplitude (VIBCAMP), with 283.3 nmol/kg Darifenacin producing a 35% inhibition, with a maximum inhibition of approximately 50-55%. Intravenous injection of 0.1 mg/kg Darifenacin in female Sprague-Dawley rats reduced bladder afferent activity in Aδ and C fibers, where the reduction in afferent spikes may be more pronounced in C fibers than in Aδ fibers.
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• In Vitro:
  Darifenacin increased the accumulation of R123 (P-gp probe) in a concentration-dependent manner in MDCK cells. Darifenacin stimulated ATPase activity in P-gp membranes in a concentration-dependent manner with an estimated ED50 = 1.6 μM. 100 nM Darifenacin showed higher permeability in the basolateral to apical direction, leading to an exocytosis ratio of ~2.6 in BBMEC monolayer cells.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

mAChR, UK-88525, UK88525

Compound Identifiers

PubChem CID

444031