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

货号:A666517 同义名: Rec-7-0040;DW61

Flavoxate HCl is a competitive AChR antagonist with IC50 of 12.2 μM, used as a muscle relaxant.

Flavoxate HCl 化学结构 CAS号:3717-88-2
Flavoxate HCl 化学结构
CAS号:3717-88-2
Flavoxate HCl 3D分子结构
CAS号:3717-88-2
Flavoxate HCl 化学结构 CAS号:3717-88-2
Flavoxate HCl 3D分子结构 CAS号:3717-88-2
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Flavoxate HCl 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]}
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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 ++++

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 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 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 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 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 技术信息

CAS号3717-88-2
分子式C24H26ClNO4
分子量 427.92
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

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

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

动物实验配方
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