| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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| 体外研究 (In Vitro) |
在人成纤维细胞中,fluphenazine decanoate 对弓形虫具有作用,IC50 值为 1.7 mM[1]。
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| 体内研究 (In Vivo) |
在猴模型中,长期使用抗精神病药物氟奋乃静癸酸酯(0.22 mg/kg,然后 0.33 mg/kg;肌肉注射;每 3 周 8 次)可增加多巴胺敏感性 [2]。为了建立人类迟发性运动障碍的药理学模型,氟奋乃静癸酸酯(25 mg/kg;肌肉注射;每三周六次;24周)引起大鼠口腔运动[3]。在成年雄性大鼠中,氟奋乃静癸酸酯(1、2、3 mg/kg/d;皮下注射;60 天)会导致促性腺激素引起高催乳素血症,并具有抗生育作用[4]。
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| 动物实验 |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (250 g) [3]
Doses: 25 mg/kg Route of Administration: intramuscularinjection of hind limbs; 24-week Experimental Results: Result in spontaneous chewing movements and mandibular tremors. Animal/Disease Models: adult male rats [4] Doses: 1, 2, 3 mg/kg/d Route of Administration: 10:00-12:00 h subcutaneous injection; 60-day Experimental Results: On the 60th day, serum prolactin levels increased High, serum LH and FSH levels are suppressed. The level of hypothalamic tyrosine hydroxylase increases and chromatin decondensation is enhanced, leading to DNA denaturation. |
| 参考文献 |
[1]. Goodwin DG, et al. Evaluation of five antischizophrenic agents against Toxoplasma gondii in human cell cultures. J Parasitol. 2011 Feb;97(1):148-51.
[2]. Lifshitz K, et al. Effects of dopamine agonists on Cebus apella monkeys with previous long-term exposure to fluphenazine. Biol Psychiatry. 1997 Mar 15;41(6):657-67. [3]. Stoessl AJ, et al. Chronic neuroleptic-induced mouth movements in the rat: suppression by CCK and selective dopamine D1 and D2 receptor antagonists. Psychopharmacology (Berl). 1989;98(3):372-9. [4]. Gill-Sharma MK, et al. Antifertility effects of fluphenazine in adult male rats. J Endocrinol Invest. 2003 Apr;26(4):316-26. |
| 其他信息 |
Fluphenazine decanoate is a prodrug of fluphenazine, an antipsychotic drug used to treat psychotic symptoms in patients with schizophrenia. It is a phenothiazine antipsychotic, a prodrug, and a dopaminergic antagonist. It belongs to the phenothiazine class of compounds, decanoates, organofluorine compounds, and N-alkylpiperazines. Its function is related to that of fluphenazine. Fluphenazine decanoate is the decanoate form of fluphenazine, a phenothiazine drug with antipsychotic activity. Fluphenazine decanoate works by blocking postsynaptic dopamine D2 receptors in the limbic system, cortical system, and basal ganglia. This blocks the action of dopamine, thereby reducing hallucinations and delusions associated with schizophrenia.
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| 分子式 |
C32H44F3N3O2S
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|---|---|
| 分子量 |
591.77
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| 精确质量 |
591.311
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| CAS号 |
5002-47-1
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| 相关CAS号 |
Fluphenazine dihydrochloride;146-56-5;Fluphenazine decanoate dihydrochloride;2376-65-0
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| PubChem CID |
3388
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| 外观&性状 |
Light yellow to yellow <30°C solid powder,>32°C liquid
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| 密度 |
1.149 g/cm3
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| 沸点 |
658.1ºCat 760 mmHg
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| 熔点 |
30-32°
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| 闪点 |
351.8ºC
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| 折射率 |
1.537
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| LogP |
7.94
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| tPSA |
61.32
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| 氢键供体(HBD)数目 |
0
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| 氢键受体(HBA)数目 |
9
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| 可旋转键数目(RBC) |
16
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| 重原子数目 |
41
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| 分子复杂度/Complexity |
765
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| 定义原子立体中心数目 |
0
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| InChi Key |
VIQCGTZFEYDQMR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H44F3N3O2S/c1-2-3-4-5-6-7-8-14-31(39)40-24-23-37-21-19-36(20-22-37)17-11-18-38-27-12-9-10-13-29(27)41-30-16-15-26(25-28(30)38)32(33,34)35/h9-10,12-13,15-16,25H,2-8,11,14,17-24H2,1H3
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| 化学名 |
2-[4-[3-[2-(trifluoromethyl)phenothiazin-10-yl]propyl]piperazin-1-yl]ethyl decanoate
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| HS Tariff Code |
2934.99.9001
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 溶解度 (体外实验) |
DMSO : ~125 mg/mL (~211.23 mM)
Ethanol : ~50 mg/mL (~84.49 mM) |
|---|---|
| 溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 1.08 mg/mL (1.83 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将100 μL 10.8 mg/mL澄清的DMSO储备液加入到400 μL PEG300中,混匀;再向上述溶液中加入50 μL Tween-80,混匀;然后加入450 μL生理盐水定容至1 mL。 *生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。 配方 2 中的溶解度: ≥ 1.08 mg/mL (1.83 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 例如,若需制备1 mL的工作液,可将 100 μL 10.8 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中,混匀。 *20% SBE-β-CD 生理盐水溶液的制备(4°C,1 周):将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中,得到澄清溶液。 View More
配方 3 中的溶解度: ≥ 1.08 mg/mL (1.83 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6898 mL | 8.4492 mL | 16.8985 mL | |
| 5 mM | 0.3380 mL | 1.6898 mL | 3.3797 mL | |
| 10 mM | 0.1690 mL | 0.8449 mL | 1.6898 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
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 ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00356200 | TERMINATEDWITH RESULTS | Drug: Fluphenazine Decanoate
Drug: Placebo |
Psoriasis | Tufts Medical Center | 2006-07 | Phase 2 |
| NCT05766007 | RECRUITING | Antipsychotic Agents Breastfeeding Drug Exposure Via Breast Milk Drug Exposure in Utero |
University of Liverpool | 2023-08-01 | ||
| NCT00014001 | COMPLETED | Drug: perphenazine Drug: olanzapine Drug: quetiapine |
Schizophrenia | National Institute of Mental Health (NIMH) | 2000-12 | Phase 4 |
| NCT02203786 | COMPLETEDWITH RESULTS | Drug: Haloperidol Drug: Fluphenazine Drug: Dexedrine |
Pathological Gambling | Centre for Addiction and Mental Health | 2009-09 | Phase 2 |
| NCT01323205 | COMPLETED | Drug: JNJ-40411813 Drug: JNJ-40411813 Drug: Placebo Drug: Antipsychotic medication |
Schizophrenia | Janssen Research & Development, LLC | 2011-05 | Phase 2 |