货号:A211196
同义名:
UK-88525 hydrobromide; Darifenacin(hydrobromide)
Darifenacin HCl 是一种 M3 选择性拮抗剂(pKi = 8.9),具有抗胆碱能及抗痉挛作用,常用于尿失禁及膀胱过度活跃的研究。


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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 |
95% | |||||||||||||||||
| (-)-Huperzine A |
++++
AChE (G4 form), Ki: 7 nM |
98% | |||||||||||||||||
| Galanthamine HBr |
++
AChE, IC50: 0.35 μM |
98% | |||||||||||||||||
| Trospium chloride | ✔ | 99% | |||||||||||||||||
| Tiotropium Bromide Monohydrate | ✔ | 97% | |||||||||||||||||
| Gallamine Triethiodide |
+
AChR, IC50: 68.0 μM |
98% | |||||||||||||||||
| Hexamethonium Bromide | ✔ | 99% | |||||||||||||||||
| Pancuronium dibromide | ✔ | 98% | |||||||||||||||||
| Neostigmine bromide | ✔ | 98% | |||||||||||||||||
| Orphenadrine citrate | ✔ | 98% | |||||||||||||||||
| Oxybutynin | ✔ | 98% | |||||||||||||||||
| Irsogladine | ✔ | PDE | 99% | ||||||||||||||||
| Pyridostigmine bromide | ✔ | 99+% | |||||||||||||||||
| Rivastigmine |
+
AChR, IC50: 5.5 μM |
98% | |||||||||||||||||
| Paroxetine HCl | ✔ | 99% | |||||||||||||||||
| Rocuronium Bromide | ✔ | 98% | |||||||||||||||||
| Tropicamide |
+++
M4 mAChR, IC50: 8 nM |
98% | |||||||||||||||||
| Diphenmanil methylsulfate | ✔ | 97% | |||||||||||||||||
| Umeclidinium bromide | ✔ | 95% | |||||||||||||||||
| Otilonium bromide | ✔ | 98% | |||||||||||||||||
| Flavoxate HCl |
+
mAChR, IC50: 12.2 μM |
99% | |||||||||||||||||
| Ipratropium bromide | ✔ | 98% | |||||||||||||||||
| Diphenidol HCl | ✔ | 98% | |||||||||||||||||
| Darifenacin hydrobromide |
++++
M3 mAChR, pKi: 8.9 |
98% | |||||||||||||||||
| Aclidinium Bromide |
++++
M2 mAChR, Ki: 0.1 nM M4 mAChR, Ki: 0.21 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。 | |||||||||||||||||||
| 靶点 |
|
| 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]. |
| 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 |
|
| CAS号 | 133099-07-7 |
| 分子式 | C28H31BrN2O2 |
| 分子量 | 507.46 |
| SMILES Code | O=C(C(C1=CC=CC=C1)([C@H]2CN(CC2)CCC3=CC4=C(C=C3)OCC4)C5=CC=CC=C5)N.Br |
| MDL No. | MFCD08141803 |
| 别名 | UK-88525 hydrobromide; Darifenacin(hydrobromide); UK 88525-04; UK-88525; Darifenacin HBr; UK-88525(hydrobromide) |
| 运输 | 蓝冰 |
| InChI Key | UQAVIASOPREUIT-VQIWEWKSSA-N |
| Pubchem ID | 444030 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, room temperature |
| 溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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