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Darifenacin (UK-88525) is a muscarinic receptor M3 antagonist with anticonvulsant activity and can be used to study urinary incontinence and overactive bladder.

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $30 | In Stock | |
| 5 mg | $59 | In Stock | |
| 10 mg | $94 | In Stock | |
| 25 mg | $172 | In Stock | |
| 50 mg | $277 | In Stock | |
| 100 mg | $416 | In Stock | |
| 200 mg | $593 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $75 | In Stock |
| Description | Darifenacin (UK-88525) is a muscarinic receptor M3 antagonist with anticonvulsant activity and can be used to study urinary incontinence and overactive bladder. |
| Targets&IC50 | ATPase activity (P-gp membranes:1.6 μM (ED50) |
| In vitro | Darifenacin increased the accumulation of R123 (P-gp probe) in a concentration-dependent manner in MDCK cells. [1] Darifenacin stimulated ATPase activity in P-gp membranes in a concentration-dependent manner with an estimated ED50 = 1.6 μM. [1] 100 nM Darifenacin showed higher permeability in the basolateral to apical direction, leading to an exocytosis ratio of ~2.6 in BBMEC monolayer cells. [1] |
| 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%. [2] 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. [3] |
| Synonyms | UK-88525, UK88525 |
| Molecular Weight | 426.55 |
| Formula | C28H30N2O2 |
| Cas No. | 133099-04-4 |
| Smiles | C(C(N)=O)([C@H]1CN(CCC=2C=C3C(=CC2)OCC3)CC1)(C4=CC=CC=C4)C5=CC=CC=C5 |
| Storage | store at low temperature,keep away from direct sunlight | store at -20°C | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (187.55 mM.), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.74 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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