1-(4-Chlorobenzhydryl)piperazine
(Synonyms: 1-(4-氯二苯甲基)哌嗪) 目录号 : GC49294An inactive metabolite of meclizine and chlorcyclizine
Cas No.:303-26-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
1-(4-Chlorobenzhydryl)piperazine is an inactive metabolite of meclizine and chlorcyclizine .1,2 It has also been found as an impurity in commercial preparations of hydroxyzine and cetirizine .3,4 1-(4-Chlorobenzhydryl)piperazine has been used in the synthesis of voltage-gated sodium channel 1.7 (Nav1.7) inhibitors, anticancer agents, and antihistamines.5,6,7
1.Gaertner, H.J., Breyer, U., and Liomin, G.Chronic administration of chlorcyclizine and meclizine to rats: Accumulation of a metabolite formed by piperazine ring cleavageJ. Pharmacol. Exp. Ther.185(2)195-201(1973) 2.Kuntzman, R., Klutch, A., Tsai, I., et al.Physiological distribution and metabolic inactivation of chlorcyclizine and cyclizineJ. Pharmacol. Exp. Ther.149(1)29-35(1965) 3.Simpson, D., Skellern, G.G., and Miller, J.H.Method for the control of known impurities in hydroxyzine hydrochlorideJ. Pharm. Biomed. Anal.14(8-10)1371-1375(1996) 4.Javid, F.S., Shafaat, A., and Zarghi, A.Determination of cetirizine and its impurities in bulk and tablet formulation using a validated capillary zone electrophoretic methodJ. Anal. Chem.69(5)442-447(2014) 5.Back, S.K., Kam, Y.L., Oh, J.A., et al.Synthesis and evaluation of (4-chlorobenzhydryl) piperazine amides as sodium channel Nav1.7 inhibitorsBull. Korean Chem. Soc.36(9)2290-2297(2015) 6.Yarim, M., Koksal, M., Durmaz, I., et al.Cancer cell cytotoxicities of 1-(4-substitutedbenzoyl)-4-(4-chlorobenzhydryl)piperazine derivativesInt. J. Mol. Sci.13(7)8071-8085(2012) 7.Narsaiah, A.V., and Narssimha, P.Efficient synthesis of antihistamines clocinizine and chlorcyclizineMed. Chem. Res.21538-541(2012)
Cas No. | 303-26-4 | SDF | |
别名 | 1-(4-氯二苯甲基)哌嗪 | ||
Canonical SMILES | ClC1=CC=C(C(N2CCNCC2)C3=CC=CC=C3)C=C1 | ||
分子式 | C17H19ClN2 | 分子量 | 286.8 |
溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:4): 0.2 mg/ml,Ethanol: 25 mg/ml | 储存条件 | -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.4868 mL | 17.4338 mL | 34.8675 mL |
5 mM | 0.6974 mL | 3.4868 mL | 6.9735 mL |
10 mM | 0.3487 mL | 1.7434 mL | 3.4868 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Cancer cell cytotoxicities of 1-(4-substitutedbenzoyl)-4-(4-chlorobenzhydryl)piperazine derivatives
Int J Mol Sci 2012;13(7):8071-8085.PMID:22942690DOI:10.3390/ijms13078071.
A series of novel 1-(4-substitutedbenzoyl)-4-(4-chlorobenzhydryl)piperazine derivatives 5a-g was designed by a nucleophilic substitution reaction of 1-(4-Chlorobenzhydryl)piperazine with various benzoyl chlorides and characterized by elemental analyses, IR and (1)H nuclear magnetic resonance spectra. Cytotoxicity of the compounds was demonstrated on cancer cell lines from liver (HUH7, FOCUS, MAHLAVU, HEPG2, HEP3B), breast (MCF7, BT20, T47D, CAMA-1), colon (HCT-116), gastric (KATO-3) and endometrial (MFE-296) cancer cell lines. Time-dependent cytotoxicity analysis of compound 5a indicated the long-term in situ stability of this compound. All compounds showed significant cell growth inhibitory activity on the selected cancer cell lines.