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氢溴酸达非那新 /Darifenacin hydrobromide {[allProObj[0].p_purity_real_show]}

货号:A211196 同义名: UK-88525 hydrobromide;Darifenacin (hydrobromide)

Darifenacin hydrobromide is a M3-selective antagonist with pKi of 8.9, an anticholinergic and antispasmotic agent used to treat urinary incontinence and overactive bladder syndrome.

Darifenacin hydrobromide 化学结构 CAS号:133099-07-7
Darifenacin hydrobromide 化学结构
CAS号:133099-07-7
Darifenacin hydrobromide 3D分子结构
CAS号:133099-07-7
Darifenacin hydrobromide 化学结构 CAS号:133099-07-7
Darifenacin hydrobromide 3D分子结构 CAS号:133099-07-7
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Darifenacin hydrobromide 纯度/质量文件 产品仅供科研

货号:A211196 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 AChE AChR mAChR nAChR 其他靶点 纯度
Donepezil +++

hAChE, IC50: 11.6 nM

bAChE, IC50: 8.12 nM

98%
Loganin ++

AChE, IC50: 3.95 μM

99%+
topride HCl ++

AChE, IC50: 2.04 μM

98%
Dehydroevodiamine HCl 99%+
Jatrorrhizine ++

AChE, IC50: 872 nM

99%+
Palmatine ++

AChE, IC50: 0.51 μM

98%
(-)-Huperzine A ++++

AChE (G4 form), Ki: 7 nM

98%
Galanthamine HBr ++

AChE, IC50: 0.35 μM

98%
Trospium chloride 99%
Tiotropium Bromide Monohydrate 98+%
Gallamine Triethiodide +

AChR, IC50: 68.0 μM

98%
Hexamethonium Bromide 99%
Pancuronium dibromide 98%
Neostigmine bromide 98%
Orphenadrine citrate 98%
Oxybutynin 98%
Irsogladine PDE 98%
Pyridostigmine bromide 99+%
Rivastigmine +

AChR, IC50: 5.5 μM

98%
Paroxetine hydrochloride 97%
Rocuronium Bromide 98%
Tropicamide +++

M4 mAChR, IC50: 8 nM

98%
Diphenmanil methylsulfate 98%
Umeclidinium bromide 95%
Otilonium bromide 98%
Flavoxate HCl +

mAChR, IC50: 12.2 μM

98%
Ipratropium bromide 98%
Diphenidol HCl 98%
Darifenacin hydrobromide ++++

M3 mAChR, pKi: 8.9

98%
Aclidinium Bromide ++++

M4 mAChR, Ki: 0.21 nM

M2 mAChR, Ki: 0.1 nM

98%
Oxybutynin chloride 99%
Pentoxyverine citrate 98%
Solifenacin 98%
Catharanthine 98%
Benzethonium chloride +++

α4β2 nAChRs, IC50: 49 nM

α7 nAChRs, IC50: 122 nM

99+%
Vinblastine sulfate +

nAChR, IC50: 8.9 μM

99%
PNU-120596 ++

α7 nAChR, EC50: 216 nM

99+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Darifenacin hydrobromide 生物活性

靶点
  • mAChR

    M3 mAChR, pKi:8.9

描述 Darifenacin hydrobromide is a selective M3 muscarinic receptor antagonist with pKi of 8.5[3]. Concentration-dependent increases in ATPase activity was observed in P-gp (P-glycoprotein) membranes following darifenacin exposure (0-10 µM) with an estimated ED50 value of 1.6 μM[4]. 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[5].

Darifenacin hydrobromide 参考文献

[1]Miller DW, Hinton M, Chen F. Evaluation of drug efflux transporter liabilities of darifenacin in cell culture models of the blood-brain and blood-ocular barriers. Neurourol Urodyn. 2011 Nov;30(8):1633-8.

[2]Hegde SS, Choppin A, et al. Functional role of M2 and M3 muscarinic receptors in the urinary bladder of rats in vitro and in vivo. Br J Pharmacol. 1997 Apr;120(8):1409-18.

[3]Hegde SS, Choppin A, Bonhaus D, Briaud S, Loeb M, Moy TM, Loury D, Eglen RM. Functional role of M2 and M3 muscarinic receptors in the urinary bladder of rats in vitro and in vivo. Br J Pharmacol. 1997 Apr;120(8):1409-18.

[4]Miller DW, Hinton M, Chen F. Evaluation of drug efflux transporter liabilities of darifenacin in cell culture models of the blood-brain and blood-ocular barriers. Neurourol Urodyn. 2011 Nov;30(8):1633-8.

[5]Iijima K, De Wachter S, Wyndaele JJ. Effects of the M3 receptor selective muscarinic antagonist darifenacin on bladder afferent activity of the rat pelvic nerve. Eur Urol. 2007 Sep;52(3):842-7.

Darifenacin hydrobromide 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.85mL

1.97mL

0.99mL

19.71mL

3.94mL

1.97mL

Darifenacin hydrobromide 技术信息

CAS号133099-07-7
分子式C28H31BrN2O2
分子量 507.462
别名 UK-88525 hydrobromide;Darifenacin (hydrobromide);UK 88525-04;UK-88525;Darifenacin HBr
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

DMSO: 35 mg/mL(68.97 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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