Darifenacin HBr (UK88525)

Alias: UK-88525; Darifenacin; Emselex; Enablex.UK 88525; UK88525;Darifenacin HBr

Cat No.:V1171 Purity: ≥98%

COA Product Data Instructions for use SDS

Darifenacin HBr (formerly known as UK-88525;Emselex; Enablex),the hydrobromide salt ofDarifenacin, is a approved medication used to treat urinary incontinence and overactive bladder.

Darifenacin HBr (UK88525) Chemical Structure CAS No.: 133099-07-7
Product category: AChR Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of Darifenacin HBr (UK88525):

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Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

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J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

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Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Biological Data

Product Description

Darifenacin HBr (formerly known as UK-88525; Emselex; Enablex), the hydrobromide salt of Darifenacin, is a approved medication used to treat urinary incontinence and overactive bladder. It acts as a selective M3 muscarinic receptor antagonist with pKi of 8.9. Darifenacin exerts non-parallel rightward displacement of the agonist curve and also significant depression of the maximum response (+)-cis-Dioxolane produced concentration-dependent contraction of the isolated bladder of rat. Darifenacin produces a concentration dependent increase in R123 (P-gp probe) accumulation in MDCK cells. Darifenacin stimulates ATPase activity in P-gp membrane in a clear concentration dependent response manner with an estimated ED50 value of 1.6 µM.

Biological Activity I Assay Protocols (From Reference)

ln Vitro

In vitro activity: Darifenacin exerts non-parallel rightward displacement of the agonist curve and also significant depression of the maximum response (+)-cis-Dioxolane produced concentration-dependent contraction of the isolated bladder of rat. Darifenacin produces a concentration dependent increase in R123 (P-gp probe) accumulation in MDCK cells. Darifenacin stimulates ATPase activity in P-gp membrane in a clear concentration dependent response manner with an estimated ED50 value of 1.6 µM. Darifenacin (100 nM) shows a significantly greater permeability for darifenacin in the basolateral to apical direction resulting in an efflux ratio in BBMEC monolayers of approximately 2.6.

ln Vivo

Darifenacin produces dose-dependent inhibition of amplitude of volume-induced bladder contractions(VIBCAMP), producing 35% inhibition at dose of 283.3 nmol/kg and maximal inhibition of approximately 50–55%. Darifenacin (0.1 mg/kg i.v.) reduces bladder afferent activity in both Aδ and C fibers in female Sprague-Dawley rats, the decrease in afferent spikes in C fibers may be more pronounced than that in Aδ fibers. Darifenacin (7.5 mg and 15 mg, daily) reduces the number of incontinence episodes per week from baseline by 67.7% and 72.8% respectively compared with 55.9% with placebo in patients with overactive bladder (OAB). Darifenacin (7.5 mg and 15 mg, daily) also shows significantly superior to placebo for improvements in micturition frequency, bladder capacity, frequency of urgency, severity of urgency and number of incontinence episodes leading to a change in clothing or pads in patients with overactive bladder (OAB).

Animal Protocol

0.1 mg/kg i.v.

Rats

References

Br J Pharmacol.1997 Apr;120(8):1409-18;Neurourol Urodyn.2011 Nov;30(8):1633-8.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C28H30N2O2.HBR

Molecular Weight

507.46

CAS #

133099-07-7

Related CAS #

(±)-Darifenacin;133033-93-9;Darifenacin;133099-04-4

SMILES

O=C(C(C1=CC=CC=C1)([C@@H]2CCN(CCC3=CC4=C(OCC4)C=C3)C2)C5=CC=CC=C5)N.Br

InChi Key

UQAVIASOPREUIT-VQIWEWKSSA-N

InChi Code

InChI=1S/C28H30N2O2.BrH/c29-27(31)28(23-7-3-1-4-8-23,24-9-5-2-6-10-24)25-14-17-30(20-25)16-13-21-11-12-26-22(19-21)15-18-32-26;/h1-12,19,25H,13-18,20H2,(H2,29,31);1H/t25-;/m1./s1

Chemical Name

2-[(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-diphenylacetamide hydrobromide

Synonyms

UK-88525; Darifenacin; Emselex; Enablex.UK 88525; UK88525;Darifenacin HBr

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO:117 mg/mL (230.5 mM)

Water:<1 mg/mL

Ethanol:<1 mg/mL

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.9706 mL	9.8530 mL	19.7060 mL
	5 mM	0.3941 mL	1.9706 mL	3.9412 mL
	10 mM	0.1971 mL	0.9853 mL	1.9706 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

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The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Biological Data

Effects of (a) methoctramine and (b) darifenacin on the re-contractile concentration-effect curve to (+)-cis-dioxolane obtained after elevation of adenylyl cyclase activity following preferential alkylation of M3 muscarinic receptors.Br J Pharmacol.1997 Apr;120(8):1409-18.

Darifenacin HBr — Effects of muscarinic receptor antagonists on (a) amplitude of volume-induced bladder contractions (VIBCAMP) (b) mean arterial pressure in urethane anaesthetized rats.Br J Pharmacol.1997 Apr;120(8):1409-18.