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奥替溴铵 /Otilonium bromide {[allProObj[0].p_purity_real_show]}

货号:A237499 同义名: Octylonium bromide;SP63

Otilonium bromide is an mAchR antagonist used world-wide for the treatment of irritable bowel syndrome.

Otilonium bromide 化学结构 CAS号:26095-59-0
Otilonium bromide 化学结构
CAS号:26095-59-0
Otilonium bromide 3D分子结构
CAS号:26095-59-0
Otilonium bromide 化学结构 CAS号:26095-59-0
Otilonium bromide 3D分子结构 CAS号:26095-59-0
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Otilonium bromide 纯度/质量文件 产品仅供科研

货号:A237499 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 +++

α7 nAChRs, IC50: 122 nM

α4β2 nAChRs, IC50: 49 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。

Otilonium bromide 生物活性

靶点
  • mAChR

描述 Otilonium bromide (OB) is a smooth muscle relaxant used in the treatment of irritable bowel syndrome. Otilonium bromide inhibited the generation of ACh-induced calcium signals in a dose dependent manner (IC50=880 nM)[3]. In experiments with recordings in the same cells of whole-cell IDMPP, Na+ currents (INa) and Ca2+ currents (ICa), 1 mM otilonium blocked 87% IDMPP, 7% INa and 13% ICa. Otilonium inhibited the K+-evoked catecholamine secretory response of superfused bovine chromaffin cells with an IC50 of 10 mM and inhibited the secretory responses induced by 10 s pulses of 50 mM DMPP with an IC50 of 7.4 nM[4].

Otilonium bromide 参考文献

[1]Martinez-Cutillas M, Gil V, et al. Mechanisms of action of otilonium bromide (OB) in human cultured smooth muscle cells and rat colonic strips. Neurogastroenterol Motil. 2013 Dec;25(12):e803-12.

[2]Forte E, Pizzoferrato M, et al. The use of anti-spasmodics in the treatment of irritable bowel syndrome: focus on otilonium bromide. Eur Rev Med Pharmacol Sci. 2012 Jan;16(1):25-37.

[3]Lindqvist S, Hernon J, Sharp P, Johns N, Addison S, Watson M, Tighe R, Greer S, Mackay J, Rhodes M, Lewis M, Stebbings W, Speakman C, Evangelista S, Johnson I, Williams M. The colon-selective spasmolytic otilonium bromide inhibits muscarinic M(3) receptor-coupled calcium signals in isolated human colonic crypts. Br J Pharmacol. 2002 Dec;137(7):1134-42.

[4]Gandía L, Villarroya M, Lara B, Olmos V, Gilabert JA, López MG, Martínez-Sierra R, Borges R, García AG. Otilonium: a potent blocker of neuronal nicotinic ACh receptors in bovine chromaffin cells. Br J Pharmacol. 1996 Feb;117(3):463-470.

Otilonium bromide 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.77mL

0.35mL

0.18mL

8.87mL

1.77mL

0.89mL

17.74mL

3.55mL

1.77mL

Otilonium bromide 技术信息

CAS号26095-59-0
分子式C29H43BrN2O4
分子量 563.567
别名 Octylonium bromide;SP63;Octylonium;Otilonium (bromide)
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,Store in freezer, under -20°C

溶解度

DMSO: 50 mg/mL(88.72 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: 100 mg/mL(177.44 mM)

动物实验配方

PO 0.5% CMC-Na 100 mg/mL suspension

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