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/ Flavoxate HCl/盐酸黄酮哌酯

Flavoxate HCl/盐酸黄酮哌酯 {[allProObj[0].p_purity_real_show]}

货号：A666517 同义名： Rec-7-0040; DW61

Flavoxate HCl是一种竞争性乙酰胆碱受体（AChR）拮抗剂，IC50为12.2 μM，常用于作为肌肉松弛剂。

Flavoxate HCl/盐酸黄酮哌酯 化学结构 CAS号：3717-88-2
Flavoxate HCl/盐酸黄酮哌酯 化学结构
CAS号：3717-88-2
Flavoxate HCl/盐酸黄酮哌酯 3D分子结构
CAS号：3717-88-2
Flavoxate HCl/盐酸黄酮哌酯 化学结构 CAS号：3717-88-2
Flavoxate HCl/盐酸黄酮哌酯 3D分子结构 CAS号：3717-88-2
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Flavoxate HCl/盐酸黄酮哌酯 纯度/质量文件 产品仅供科研

货号：A666517 标准纯度： {[allProObj[0].p_purity_real_show]}
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

 		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。

Flavoxate HCl/盐酸黄酮哌酯 生物活性

靶点

  • mAChR

    mAChR, IC50:12.2 μM
描述 Flavoxate Hydrochloride is a muscarinic AChR antagonist. It has been reported that flavoxate causes a concentration-dependent relaxation of the tension elicited by muscarinic stimulation (IC50=35 μM) or 5 mM extracellular Ca2+ (IC50=83 μM) in rat detrusor. And flavoxate caused a concentration-dependent relaxation of human urinary bladder precontracted by K+ with much higher potency (IC50=2 μM)[3]. Flavoxate (10-8-10-5 M) inhibited cAMP formation in a concentration-dependent manner. Flavoxate (3 mg/kg, i.v.) completely abolished rhythmic bladder contractions in vehicle-pretreated rats, but not in PTX-pretreated (pertussis toxin ) rats[4].

Flavoxate HCl/盐酸黄酮哌酯 细胞实验

Cell Line
Concentration Treated Time Description References
human detrusor myocytes 10 μM To investigate the effects of Flavoxate on voltage-dependent Ba2+ inward currents, results showed Flavoxate inhibited the peak amplitude in a voltage- and concentration-dependent manner Br J Pharmacol. 2005 Sep;146(1):25-32.
PC12 cells 100 μM 30 min To investigate the inhibitory effect of Flavoxate on calcium channels in PC12 cells and its impact on cytotoxicity and apoptosis. Results showed that Flavoxate pretreatment increased cytotoxicity and apoptotic index, and reduced neurite outgrowth compared to the control group. Bosn J Basic Med Sci. 2012 Feb;12(1):20-5.

Flavoxate HCl/盐酸黄酮哌酯 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00440739 Pain Phase 4 Completed - Thailand ... 展开 >> Faculty of Medicine Siriraj Hospital, Mahidol University Bangkok, Thailand, 10700 收起 <<
NCT00992238 Healthy Phase 1 Completed - United States, North Dakota ... 展开 >> PRACS Institute, Ltd Fargo, North Dakota, United States, 58104 收起 <<

Flavoxate HCl/盐酸黄酮哌酯 参考文献

[1]Dansette PM, Jaoen M, et al. HMG-CoA reductase activity in human liver microsomes: comparative inhibition by statins. Exp Toxicol Pathol. 2000 May;52(2):145-8.

[2]Kimura Y, Sasaki Y, et al. Mechanisms of the suppression of the bladder activity by flavoxate. Int J Urol. 1996 May;3(3):218-27.

[3]Tomoda T, Aishima M, Takano N, Nakano T, Seki N, Yonemitsu Y, Sueishi K, Naito S, Ito Y, Teramoto N. The effects of flavoxate hydrochloride on voltage-dependent L-type Ca2+ currents in human urinary bladder. Br J Pharmacol. 2005 Sep;146(1):25-32.

[4]Oka M, Kimura Y, Itoh Y, Sasaki Y, Taniguchi N, Ukai Y, Yoshikuni Y, Kimura K. Brain pertussis toxin-sensitive G proteins are involved in the flavoxate hydrochloride-induced suppression of the micturition reflex in rats. Brain Res. 1996 Jul 15;727(1-2):91-8.

Flavoxate HCl/盐酸黄酮哌酯 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.68mL

2.34mL

1.17mL

23.37mL

4.67mL

2.34mL

Flavoxate HCl/盐酸黄酮哌酯 技术信息

CAS号3717-88-2
分子式C24H26ClNO4
分子量 427.92
SMILES Code O=C(C1=C2C(C(C(C)=C(C3=CC=CC=C3)O2)=O)=CC=C1)OCCN4CCCCC4.Cl
MDL No. MFCD00072099
别名 Rec-7-0040; DW61; Flavoxate HCl, Flavoxate hydrochloride, DW-61, Rec-7-0040; Rec 7/0040; Flavoxate (hydrochloride); NSC-114649; Flavoxate hydrochloride
运输蓝冰
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: 3 mg/mL(7.01 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

H2O: 5 mg/mL(11.68 mM)，配合低频超声助溶

Tags: Flavoxate | 3717-88-2 | Rec-7-0040 | DW61 | DW61 | DW 61 | DW-61 | PDE Inhibitor | Metabolic Enzyme/Protease | Membrane Transporter/Ion Channel | GPCR/G Protein | Neuronal Signaling | Phosphodiesterase (PDE) | Calcium Channel | mAChR | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Flavoxate HCl/盐酸黄酮哌酯 纯度/质量文件 | Flavoxate HCl/盐酸黄酮哌酯 亚型比较 | Flavoxate HCl/盐酸黄酮哌酯 生物活性 | Flavoxate HCl/盐酸黄酮哌酯 临床数据 | Flavoxate HCl/盐酸黄酮哌酯 参考文献 | Flavoxate HCl/盐酸黄酮哌酯 实验方案 | Flavoxate HCl/盐酸黄酮哌酯 技术信息

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