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ChemicalBook Product Catalog Biochemical Engineering Inhibitors Neuronal Signaling AChR antagonist Darifenacin hydrobromide

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Darifenacin hydrobromide NEW

$42.00 50mg

$50.00 100mg

Min. Order
Purity99.71%
Cas No133099-07-7
Supply Ability10g
Update time2024-11-19

TargetMol Chemicals Inc.

TargetMol Chemicals Inc.

5YR

United States

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Chemical Properties

Product Name	Darifenacin hydrobromide
CAS No	133099-07-7
EC-No
Min. Order
Purity	99.71%
Supply Ability	10g
Release date	2024/11/19

Product Introduction

Bioactivity

Name	Darifenacin hydrobromide
Description	Darifenacin hydrobromide (UK-88525) is a selective muscarinic receptor antagonist used to treat urinary incontinence and overactive bladder syndrome.
In vitro	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. [1] 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. [2]
In 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%. [1] 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. [3] 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). [4]
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 93 mg/mL (184 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble)
Keywords	Darifenacin hydrobromide \| Darifenacin Hydrobromide \| Darifenacin \| Muscarinic acetylcholine receptor \| UK88525 \| inhibit \| mAChR \| UK 88525 \| Inhibitor
Inhibitors Related	Adiphenine hydrochloride \| Ribavirin \| Choline chloride \| Propoxur
Related Compound Libraries	Bioactive Compound Library \| Anti-Neurodegenerative Disease Compound Library \| Membrane Protein-targeted Compound Library \| EMA Approved Drug Library \| Inhibitor Library \| FDA-Approved Drug Library \| Bioactive Compounds Library Max

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