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Darifenacin HBr(UK88525)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Darifenacin HBr(UK88525)图片
CAS NO:133099-07-7
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)507.46
FormulaC28H30N2O2.HBr
CAS No.133099-07-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 117 mg/mL (230.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Other info

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

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

SMILES Code: O=C(N)C(C1=CC=CC=C1)([C@H]2CN(CCC3=CC4=C(OCC4)C=C3)CC2)C5=CC=CC=C5.[H]Br

SynonymsUK-88525; Darifenacin; Emselex; Enablex. UK 88525; UK88525; Darifenacin HBr
实验参考方法
In 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.

In VivoDarifenacin 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 modelRats
Formulation & Dosage0.1 mg/kg i.v.
References

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