| 生物活性： |
靶点：nAChR
通路：Neuronal Signaling;Membrane Transporter&Ion Channel
背景说明：Benzethonium Chloride是有效的neuronal nicotinic acetylcholine receptors (nAChRs)抑制剂,抑制α4β2 nAChRs和α7 nAChRsM。
生物活性：Benzethonium chloride 是有效的neuronal nicotinic acetylcholine receptors (nAChRs)（神经元烟碱型乙酰胆碱受体）抑制剂，抑制α4β2 nAChRs和α7 nAChRs，IC50分别为49 nM 和 122 nM。[1]
In Vitro：Benzethonium chloride以混合竞争性和非竞争性的方式抑制α7 nAChRs中乙酰胆碱的应答，但这两种方式都不存在电压依赖响应或者使用依赖响应。[1] Benzethonium chloride降低细胞活性，其IC50在FaDu中为3.8 μM，在NIH 3T3中为42.2 μM，在C666-1中为5.3 μM，而在GM05757中为 17.0 μM 。Benzethonium chloride(9 μM)在FaDu细胞中12小时后会诱导细胞凋亡，并且激活胱天蛋白酶。 [2]
In Vivo：Benzethonium chloride(5 mg/kg)切断FaDu细胞肿瘤形成能力，延缓移植瘤的生长，并结合局部肿瘤放射疗法来治疗SCID小鼠体内的FaDu肿瘤。 [2]
细胞实验：FaDu cells were injected into the left gastrocnemius muscle of SCID mice(2.5 × 105 in 100-μL growth medium per mouse). The leg diameter of a normal mouse was <7 mm. When the tumor-plus-leg diameter reached 7.25 mm，the mice were randomized into one of the following groups:(a)PBS，(b)benzethonium chloride，(c)radiation-plus-PBS，and(d)radiation-plus-benzethonium chloride. On days 1 to 5，the mice were given one i.p. injection(100 μL bolus)daily of either PBS or benzethonium chloride(5 mg/kg in PBS).[2]
动物实验：Briefly，FaDu cells were seeded(0.3 × 106 per T-25 flask)，allowed to incubate for 1 day，and then treated with benzethonium chloride or vehicle alone(0.1% DMSO)as indicated. After 24 hours，all floating and adherent cells(using trypsin)were collected and resuspended in growth medium at a concentration of 106/mL. DiIC1(5)(40 nmol/L final concentration)and indo-1 AM(2 μmol/L final concentration)were added to the cell suspensions. The cells were incubated at 37°C for 25 minutes and propidium iodide(1 μg/mL)was then added. The cells were analyzed by flow cytometry using a Coulter Epics Elite [Beckman Coulter; DiIC1(5)excitation 633 nm，675 ± 20 nm bandpass; indo-1 AM excitation 360 nm，emission ratio 405/525 nm].[2]
数据来源文献：[1] Coates KM， et al. Br J Pharmacol， 2001， 134(4)， 871-879.
[2] Yip KW， et al. Clin Cancer Res， 2006， 12(18)， 5557-5569.
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| 其它标识： |
EC：EINECS 204-479-9
MDL：MFCD00011742
SMILES：CC(C)(C)CC(C)(C)C1=CC=C(C=C1)OCCOCC[N+](C)(C)CC2=CC=CC=C2.[Cl-]
InChIKey：UREZNYTWGJKWBI-UHFFFAOYSA-M
InChI：InChI=1S/C27H42NO2.ClH/c1-26(2,3)22-27(4,5)24-13-15-25(16-14-24)30-20-19-29-18-17-28(6,7)21-23-11-9-8-10-12-23;/h8-16H,17-22H2,1-7H3;1H/q+1;/p-1
PubChem CID：8478
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| 基本信息： |
CAS：121-54-0
中文名称：苄索氯铵
英文名称：Benzethonium Chloride
别名：苄索氯铵;海胺1622;苄己铵;季铵盐1622;
分子式：C27H42ClNO2
分子量：448.08
规格：100mg ; 250mg ; 500mg
溶解性：Soluble in Water/DMSO
纯度：≥98%
外观(性状)：White to light yellow Solid
储存条件：Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
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| 靶点： |
nAChR |
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