Fluphenazine dihydrochloride (Synonyms: 盐酸氟奋乃静)

目录号: HY-A0081 纯度: 99.89%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Fluphenazine dihydrochloride 是一种有效且具有口服活性的吩噻嗪类多巴胺受体 (dopamine receptor) 拮抗剂。Fluphenazine dihydrochloride 阻断神经元电压门控的钠离子通道 (sodium channels)。Fluphenazine dihydrochloride 主要通过拮抗中边缘、黑质纹状体和下颌结节神经通路的突触后多巴胺-2 受体来发挥作用。Fluphenazine dihydrochloride 可拮抗苯甲酸甲酯诱导的小鼠刻板咬伤，抑制小鼠攀爬行为。Fluphenazine dihydrochloride 可用于研究精神病以及与糖尿病相关的疼痛性周围神经病变，并有抑制 SARS-CoV-2 的潜力。

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Fluphenazine dihydrochloride Chemical Structure

CAS No. : 146-56-5

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规格	价格	是否有货
100 mg	￥600	In-stock
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Customer Review

Other Forms of Fluphenazine dihydrochloride:

Fluphenazine-d₈ dihydrochloride In-stock
Fluphenazine decanoate In-stock
Fluphenazine 询价
Fluphenazine dimaleate 询价
Fluphenazine hydrochloride 询价
Fluphenazine dihydrochloride (Standard) 询价

MCE 顾客使用本产品发表的 1 篇科研文献

•Dev Cell. 2024 Jul 30:S1534-5807(24)00441-6. [Abstract]

Fluphenazine dihydrochloride 相关产品

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Dopamine Receptor D₁ Receptor D₂ Receptor D₃ Receptor D₄ Receptor D₅ Receptor

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生物活性
纯度 & 产品资料
参考文献

生物活性

Fluphenazine dihydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dihydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine dihydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dihydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dihydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2^[1]^[2]^[3]^[4]^[6].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	110 μM Compound: fluphenazine	Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy	[PMID: 18788725]
HepG2	IC₅₀	4.4 μM Compound: SYSU-20913S	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay	10.1039/C3MD00397C
HUVEC	IC₅₀	38.01 μM Compound: Fluphenazine	Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay	[PMID: 34435487]
L02	IC₅₀	> 160 μM Compound: SYSU-20913S	Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay	10.1039/C3MD00397C
MCF7	IC₅₀	24.57 μM Compound: Fluphenazine	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34435487]
MDA-MB-231	IC₅₀	16.73 μM Compound: Fluphenazine	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34435487]
MDA-MB-231	IC₅₀	18.56 μM Compound: Fluphenazine	Antiproliferative activity against human drug tolerant MDA-MB-231/lapatinib cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay Antiproliferative activity against human drug tolerant MDA-MB-231/lapatinib cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay	[PMID: 34435487]

体内研究
(In Vivo)

Fluphenazine (1 mg/kg；IG，从妊娠第 6 天到第 15 天进行) dihydrochloride 会导致怀孕小鼠畸形^[5]。
Fluphenazine (0.125-1 mg/kg；IP，单剂量) dihydrochloride 拮抗哌醋甲酯引起的刻板啃咬，显着抑制攀爬行为^[6]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

510.44

Formula

C₂₂H₂₈Cl₂F₃N₃OS

CAS 号

146-56-5

性状

固体

颜色

White to off-white

中文名称

盐酸氟奋乃静

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据

细胞实验：

H₂O 中的溶解度 : 100 mg/mL (195.91 mM; 超声助溶)

DMSO 中的溶解度 : ≥ 38 mg/mL (74.45 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9591 mL	9.7955 mL	19.5909 mL
5 mM	0.3918 mL	1.9591 mL	3.9182 mL
10 mM	0.1959 mL	0.9795 mL	1.9591 mL

查看完整储备液配制表

* 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, 6 months; -20°C, 1 month (stored under nitrogen)。-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。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.07 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.07 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.07 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： PBS
Solubility: 100 mg/mL (195.91 mM); 澄清溶液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

该产品水溶性佳，请具体参考实测水 / PBS / Saline 中的溶解度数据。

您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。

纯度 & 产品资料

纯度: 99.89%

选择批次：

Data Sheet (640 KB) SDS (584 KB)

COA (193 KB) HNMR (302 KB) LCMS (96 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Zhou X, et al. The neuroleptic drug, fluphenazine, blocks neuronal voltage-gated sodium channels. Brain Res. 2006;1106(1):72-81. [Content Brief]

[2]. Nazeam J, et al. Based on Principles and Insights of COVID-19 Epidemiology, Genome Sequencing, and Pathogenesis: Retrospective Analysis of Sinigrin and ProlixinRX (Fluphenazine) Provides Off-Label Drug Candidates. SLAS Discov. 2020 Dec;25(10):1123-1140. [Content Brief]

[3]. Siragusa S, Bistas KG, Saadabadi A. Fluphenazine. 2022 May 8. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2022 Jan. [Content Brief]

[4]. Davis JL, et al. Peripheral diabetic neuropathy treated with amitriptyline and fluphenazine. JAMA. 1977 Nov 21;238(21):2291-2. [Content Brief]

[5]. Abdel-Hamid HA, et al. Teratogenic effect of diphenylhydantoin and/or fluphenazine in mice. J Appl Toxicol. 1996 May-Jun;16(3):221-5. [Content Brief]

[6]. Langwiński R, Niedzielski J. Narcotic analgesics and stereotyped behaviour in mice. Naunyn Schmiedebergs Arch Pharmacol. 1980 Jul;312(3):225-7. [Content Brief]

Fluphenazine dihydrochloride 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	1.9591 mL	9.7955 mL	19.5909 mL	48.9774 mL
	5 mM	0.3918 mL	1.9591 mL	3.9182 mL	9.7955 mL
	10 mM	0.1959 mL	0.9795 mL	1.9591 mL	4.8977 mL
	15 mM	0.1306 mL	0.6530 mL	1.3061 mL	3.2652 mL
	20 mM	0.0980 mL	0.4898 mL	0.9795 mL	2.4489 mL
	25 mM	0.0784 mL	0.3918 mL	0.7836 mL	1.9591 mL
	30 mM	0.0653 mL	0.3265 mL	0.6530 mL	1.6326 mL
	40 mM	0.0490 mL	0.2449 mL	0.4898 mL	1.2244 mL
	50 mM	0.0392 mL	0.1959 mL	0.3918 mL	0.9795 mL
	60 mM	0.0327 mL	0.1633 mL	0.3265 mL	0.8163 mL
H₂O	80 mM	0.0245 mL	0.1224 mL	0.2449 mL	0.6122 mL
H₂O	100 mM	0.0196 mL	0.0980 mL	0.1959 mL	0.4898 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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沪(浦)应急管危经许[2021]201709(QFYS)

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Fluphenazine dihydrochloride (Synonyms: 盐酸氟奋乃静)

Customer Review

Other Forms of Fluphenazine dihydrochloride:

MCE 顾客使用本产品发表的 1 篇科研文献