Zuclopenthixol

Name: Zuclopenthixol
Brand: TargetMol
SKU: T4117
Price: 173 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.82%

货号 T4117Cas号 53772-83-1

别名 珠氯噻醇, Cisordinol, cis-Clopenthixol, (Z)-Clopenthixol

Zuclopenthixol (cis-Clopenthixol) 是一种多巴胺 D1/D2受体的拮抗剂，是一种噻吨衍生物。

Zuclopenthixol

一键复制产品信息

很棒

纯度: 99.82%

货号 T4117 别名 珠氯噻醇, Cisordinol, cis-Clopenthixol, (Z)-ClopenthixolCas号 53772-83-1

Zuclopenthixol (cis-Clopenthixol) 是一种多巴胺 D1/D2受体的拮抗剂，是一种噻吨衍生物。

规格	价格	库存
25 mg	¥ 223	现货
50 mg	¥ 327	现货
100 mg	¥ 515	现货
200 mg	¥ 882	现货
500 mg	¥ 1,480	现货
1 mL x 10 mM (in DMSO)	¥ 173	现货

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COA HNMR LCMS 产品操作手册

产品介绍

Zuclopenthixol AI Summary

Zuclopenthixol demonstrates a wide range of pharmacological activities, suggesting a potential utility in various biomedical applications. It exhibits significant multidrug resistance reversal activity against the P388 murine leukemia cell line and the doxorubicin-resistant human breast carcinoma cell line MCF-7/DOX, with reversal factors of 15.0 and MDR ratios of 15.0 and 2.6, respectively. Additionally, it is effective against the SARS-CoV-2 virus, showing inhibitory activity with IC50 values between 7240.0 nM and 7244.36 nM, alongside an antiviral hit score of 0.1545 in HRCE cell assays. Pharmacokinetic properties highlight Zuclopenthixol’s high oral bioavailability at 79.0%, with a partition coefficient (logD6.5) of 2.71 and a delta logD of -0.83 when transitioning from pH 6.5 to pH 7.4. It has an ionization constant (pKa) of 8.1. The compound exhibits moderate liver toxicity but does not cause severe liver damage or acute liver toxicity. Bioactivity assays reveal that Zuclopenthixol is a potent inhibitor of human HDAC6, demonstrating high inhibition rates in enzymatic assays and an IC50 value of 3377.0 nM for custom substrate assays. It also shows activity as a serotonin 6 (5HT6) receptor antagonist, with a Ki value of 169.0 nM, and inhibits several cytochrome P450 enzymes, such as CYP2C19 and CYP3A4. Additional activities include modulating Lamin A splicing, inhibiting ubiquitin-specific proteases, and acting on various receptors like ADRA1A, ADRA2C, HTR2B, DRD2, HTR1A, and HTR2A, with varying affinities. Overall, Zuclopenthixol possesses a complex and diverse bioactivity profile, suggesting its potential in treating multidrug-resistant cancers, viral infections, and various other conditions through its multi-target interactions..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Zuclopenthixol (cis-Clopenthixol) is a thioxanthene with therapeutic actions similar to the phenothiazine antipsychotics. It is an antagonist at D1 and D2 dopamine receptors.
别名	珠氯噻醇, Cisordinol, cis-Clopenthixol, (Z)-Clopenthixol

化学信息

分子量	400.96
分子式	C₂₂H₂₅ClN₂OS
CAS No.	53772-83-1
Smiles	OCCN1CCN(CC\C=C2\c3ccccc3Sc3ccc(Cl)cc23)CC1
密度	1.289g/cm3
颜色	White
物理性状	Solid

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 250 mg/mL (623.5 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (12.47 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4940 mL	12.4701 mL	24.9401 mL	124.7007 mL
5 mM	0.4988 mL	2.4940 mL	4.9880 mL	24.9401 mL
10 mM	0.2494 mL	1.2470 mL	2.4940 mL	12.4701 mL
20 mM	0.1247 mL	0.6235 mL	1.2470 mL	6.2350 mL
50 mM	0.0499 mL	0.2494 mL	0.4988 mL	2.4940 mL
100 mM	0.0249 mL	0.1247 mL	0.2494 mL	1.2470 mL