氢溴酸达非那新 T1534

Product Introduction
Bioactivity


英文名: Darifenacin hydrobromide

描述: Darifenacin hydrobromide (UK-88525) 是一种选择性 M3 蕈毒碱受体拮抗剂，pKi 为 8.9。

体外活性: 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]

体内活性: 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]

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

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 93 mg/mL (184 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: Darifenacin hydrobromide | Darifenacin Hydrobromide | Darifenacin | Muscarinic acetylcholine receptor | UK88525 | inhibit | mAChR | UK 88525 | Inhibitor

相关产品: Nor-benzetimide | Dipivefrin hydrochloride | VU0152099 | Metoclopramide hydrochloride | Terfenadine | Clevidipine | Loganin | Peimisine | AQW051 | N-Methylcytisine

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Neurotransmitter Receptor Compound Library | Drug-induced Liver Injury (DILI) Compound Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | Neuronal Signaling Compound Library | Inhibitor Library | EMA Approved Drug Library | Bioactive Compound Library

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