苄索氯铵
货号：
IB1520
品牌：
Jinpan
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产品简介
| 有效期 | 2年 |
| 描述 | 是有效的neuronal nicotinic acetylcholine receptors (nAChRs)抑制剂，抑制α4β2 nAChRs和α7 nAChRsM。 |
| EC | EINECS 204-479-9 |
| MDL | MFCD00011742 |
| 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 |
| 别名 | 苄己铵 |
| 英文名称 | Benzethonium Chloride |
| CAS | 121-54-0 |
| 分子式 | C27H42ClNO2 |
| 分子量 | 448.08 |
| 储存条件 | -20℃ |
| 纯度 | ≥98% |
| 外观（性状） | White crystalline Powder |
| 单位 | 瓶 |
| 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] |
| SMILES | CC(C)(C)CC(C1=CC=C(OCCOCC[N+](C)(C)CC2=CC=CC=C2)C=C1)(C)C.[Cl-] |
| 靶点 | nAChR |
| 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] |
| 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, mice were randomized into one of following groups: (a) pbs, (b) benzethonium chloride, (c) radiation-plus-pbs, and (d) radiation-plus-benzethonium chloride. on days 1 to 5, given i.p. injection (100 μl bolus) daily either pbs or chloride (5 mg> |
| 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. |
| 规格 | 100mg 250mg 500mg |