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Darifenacin

🥰Excellent
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

Darifenacin

🥰Excellent
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 SizePriceAvailabilityQuantity
1 mg$30In Stock
5 mg$64In Stock
10 mg$98In Stock
25 mg$197In Stock
50 mg$297In Stock
100 mg$442In Stock
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Product Introduction

Bioactivity
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]
AliasUK-88525, UK88525
Chemical Properties
Molecular Weight426.55
FormulaC28H30N2O2
Cas No.133099-04-4
SmilesC(C(N)=O)([C@H]1CN(CCC=2C=C3C(=CC2)OCC3)CC1)(C4=CC=CC=C4)C5=CC=CC=C5
Storage & Solubility Information
Storagestore 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
1mg5mg10mg50mg
1 mM2.3444 mL11.7220 mL23.4439 mL117.2196 mL
5 mM0.4689 mL2.3444 mL4.6888 mL23.4439 mL
10 mM0.2344 mL1.1722 mL2.3444 mL11.7220 mL
20 mM0.1172 mL0.5861 mL1.1722 mL5.8610 mL
50 mM0.0469 mL0.2344 mL0.4689 mL2.3444 mL
100 mM0.0234 mL0.1172 mL0.2344 mL1.1722 mL

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TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (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 DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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