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Darifenacin hydrobromide

Catalog No. T1534 CAS 133099-07-7

Synonyms: Darifenacin HBr, UK-88525

Darifenacin hydrobromide (UK-88525) is a selective muscarinic receptor antagonist used to treat urinary incontinence and overactive bladder syndrome.

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Darifenacin hydrobromide Chemical Structure

Darifenacin hydrobromide, CAS 133099-07-7

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50 mg	In stock	$ 42.00
100 mg	In stock	$ 50.00
1 mL * 10 mM (in DMSO)	In stock	$ 30.00

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Purity: 100%

Purity: 99.71%

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Description	Darifenacin hydrobromide (UK-88525) is a selective muscarinic receptor antagonist used to treat urinary incontinence and overactive bladder syndrome.
Targets&IC50	M3 mAChR:8.9(pKi)
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]

Synonyms	Darifenacin HBr, UK-88525
Molecular Weight	505.45
Formula	C28H31BrN2O2
CAS No.	133099-07-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (184 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Hegde SS, et al. Br J Pharmacol, 1997, 120(8), 1409-1418. 2. Miller DW, et al. Neurourol Urodyn, 2011, 30(8), 1633-1638. 3. Iijima K, et al. Eur Urol, 2007, 52(3), 842-847. 4. Haab F, et al. Eur Urol, 2004, 45(4), 420-429.

Related compound libraries

This product is contained In the following compound libraries：

EMA Approved Drug Library Anti-Neurodegenerative Disease Compound Library Drug Repurposing Compound Library Membrane Protein-targeted Compound Library Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library Neuronal Signaling Compound Library ReFRAME Related Library Drug-induced Liver Injury (DILI) Compound Library

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Keywords

Darifenacin hydrobromide 133099-07-7 Neuroscience AChR Darifenacin Hydrobromide Darifenacin Darifenacin HBr Muscarinic acetylcholine receptor UK-88525 UK88525 inhibit mAChR UK 88525 Inhibitor inhibitor

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