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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 | $64 | In Stock | |
10 mg | $98 | In Stock | |
25 mg | $197 | In Stock | |
50 mg | $297 | In Stock | |
100 mg | $442 | 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 in 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] |
Alias | 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. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (187.55 mM.), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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