Home Neuronal Signaling AChR antagonist Darifenacin HBr For research use only.

Darifenacin HBr

Synonyms: UK-88525

Darifenacin HBr (UK-88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.

Darifenacin HBr Chemical Structure

Darifenacin HBr Chemical Structure

CAS: 133099-07-7

Selleck's Darifenacin HBr has been cited by 2 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK cells Function assay Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay, EC50=0.00082 μM 21310610
H292 cells Function assay Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins, EC50=0.01585 μM 21723724
HEK293 cells Function assay Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting, EC50=0.0007943 μM 25629394
CHO-K1 cells Function assay Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform, IC50=1.58489 μM 25087753
PC3 Proliferation assay 10 μM and 20 μM blockade of CHRM3 by darifenacin could effectively reduce cell proliferation 26071486
22Rv1 Proliferation assay 10 μM and 20 μM blockade of CHRM3 by darifenacin could effectively reduce cell proliferation 26071486
H1299 Proliferation assay 0.3–100 µM 72 h significantly inhibited H1299 cell proliferation in a concentration-dependent manner 23285263
Click to View More Cell Line Experimental Data

Biological Activity

Description Darifenacin HBr (UK-88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.
Targets
M3 mAChR [1]
8.9(pKi)
In vitro
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00703703 Completed Healthy Novartis|Procter and Gamble May 2008 Phase 1
NCT00921245 Completed Overactive Bladder Bayer June 2007 --
NCT00413790 Completed Healthy Novartis|Procter and Gamble November 2006 Phase 4
NCT00413426 Completed Healthy Novartis|Procter and Gamble June 2006 Phase 1
NCT00366002 Completed Overactive Bladder (OAB) Novartis|Procter and Gamble June 2006 Phase 4

Chemical lnformation & Solubility

Molecular Weight 507.46 Formula

C28H30N2O2.HBr
CAS No. 133099-07-7 SDF Download Darifenacin HBr SDF
Smiles C1CN(CC1C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N)CCC4=CC5=C(C=C4)OCC5.Br
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 117 mg/mL ( (230.56 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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