Darifenacin

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 10mM*1mL (in DMSO)
ArtNr HY-A0033-10mM
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Synonyms
UK-88525, UK 88525, UK88525
CAS No.
133099-04-4
Purity
>98%
MW
426.55
Formula
C28H30N2O2
Solubility
10 mM in DMSO
Biological Description
Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.
IC50 value: 8.9 (pKi) [1]
Target: M3 receptor
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 uM. 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 Adelta and C fibers in female Sprague-Dawley rats, the decrease in afferent spikes in C fibers may be more pronounced than that in Adelta fibers [3].
Publications
Br J Pharmacol. 2015 Dec; 172(23):5619-33.
Menge: 10mM*1mL (in DMSO)
Lieferbar: In stock
Listenpreis: 177,50 €
Preis: 177,50 €
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