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首页 / 抑制剂/激动剂 / 神经信号通路 / AChR / Darifenacin hydrobromide

氢溴酸达非那新 /Darifenacin hydrobromide 98%

货号：A211196 同义名： UK-88525 hydrobromide;Darifenacin (hydrobromide) Ambeed 开学季，买赠积分，赢豪礼

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： 98%
批次查询： 批次纯度:

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产品名称 AChE ↓ AChR ↓ mAChR ↓ nAChR ↓ 其他靶点 纯度
Donepezil +++

bAChE, IC50: 8.12 nM

hAChE, IC50: 11.6 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

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
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

Tags: Darifenacin hydrobromide | UK-88525 hydrobromide;Darifenacin (hydrobromide);UK 88525-04;UK-88525;Darifenacin HBr | AChR | AmBeed-信号通路专用抑制剂 | Darifenacin hydrobromide 纯度/质量文件 | Darifenacin hydrobromide 亚型比较 | Darifenacin hydrobromide 生物活性 | Darifenacin hydrobromide 参考文献 | Darifenacin hydrobromide 实验方案 | Darifenacin hydrobromide 技术信息

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