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Darifenacin
Catalog No. T62320Cas No. 133099-04-4
Alias UK-88525, UK88525
Darifenacin (UK-88525) is a muscarinic receptor M3 antagonist with anticonvulsant activity and can be used to study urinary incontinence and overactive bladder.
Darifenacin
Catalog No. T62320Alias UK-88525, UK88525Cas No. 133099-04-4
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 |
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Product Introduction
Bioactivity
Chemical Properties
| 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 |
Storage & Solubility Information
| 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 | ||||||||||||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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