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  2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein Autophagy Apoptosis
  3. Calcium Channel Dopamine Receptor Autophagy Apoptosis
  4. Penfluridol

Penfluridol  (Synonyms: 五氟利多; R-16341)

目錄號: HY-B1077 純度: 99.84%
COA 產(chǎn)品使用指南 技術(shù)支持

Penfluridol (R-16341) 是一種強(qiáng)效、長效、第一代具有口服活性的，二苯基丁基哌啶抗精神病藥物，可以靶向 D2 樣多巴胺受體。Penfluridol 可有效抑制 TNFα 誘導(dǎo)的 NF-κB 激活，減輕體內(nèi)關(guān)節(jié)炎和結(jié)腸炎的嚴(yán)重程度。Penfluridol 是一種 Ca2+-鈣調(diào)蛋白抑制劑。Penfluridol 抑制自噬和凋亡。Penfluridol 用于治療慢性精神分裂癥、急性精神病、抽動穢語綜合癥和自身免疫性疾病。Penfluridol 抑制糞腸球菌浮游細(xì)胞的生長，MIC 為 7.81 μg/ml。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個人用途提供產(chǎn)品和服務(wù)

Penfluridol Chemical Structure

Penfluridol Chemical Structure

CAS No. : 26864-56-2

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥566
In-stock
50 mg ￥515
In-stock
100 mg ￥800
In-stock
500 mg ￥1600
In-stock
1 g ￥2400
In-stock
5 g   詢價  
10 g   詢價  

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Customer Review

Other Forms of Penfluridol:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Penfluridol (R-16341) is a potent, long-acting, first-generation, oral diphenylbutylpiperidine antipsychotic agent by targeting D2-like dopamine receptor. Penfluridol effectively inhibits TNFα-induced NF-κB activation and alleviates the severity of arthritis and colitis in vivo. Penfluridol is a Ca2+-calmodulin inhibitor. Penfluridol induces apoptosis and autophagy. Penfluridol is used for chronic schizophrenia, acute psychosis, Tourette syndrome and autoimmune diseases. Penfluridol inhibites the growth of E. faecalis planktonic cells with the MIC of 7.81 μg/ml[1][2][3][4].

IC50 & Target[2]

D2 Receptor

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
H4 EC50
3.2 μM
Compound: 2
Induction of autophagy in human H4 cells expressing LC3 using DAPI staining after 4 hrs by fluorescence microscopic analysis
Induction of autophagy in human H4 cells expressing LC3 using DAPI staining after 4 hrs by fluorescence microscopic analysis
[PMID: 21126871]
Lewis lung carcinoma cell line IC50
4.2 μM
Compound: PFL
Cytotoxicity against mouse LLC cells harboring luciferin assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against mouse LLC cells harboring luciferin assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 30389290]
Lewis lung carcinoma cell line IC50
4.3 μM
Compound: PFL
Cytotoxicity against mouse LLC cells harboring luciferin assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against mouse LLC cells harboring luciferin assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 30389290]
Lewis lung carcinoma cell line IC50
6 μM
Compound: PFL
Cytotoxicity against mouse LLC cells harboring luciferin assessed as reduction in cell viability after 24 hrs by MTT assay
Cytotoxicity against mouse LLC cells harboring luciferin assessed as reduction in cell viability after 24 hrs by MTT assay
[PMID: 30389290]
MDA-MB-231 IC50
2.3 μM
Compound: 1
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 33039722]
MDA-MB-231 IC50
5 μM
Compound: PFL
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 30389290]
MDA-MB-231 IC50
5.1 μM
Compound: PFL
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 30389290]
MDA-MB-231 IC50
6.1 μM
Compound: PFL
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 24 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 24 hrs by MTT assay
[PMID: 30389290]
NIH3T3 IC50
6.01 μM
Compound: PFL
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 30389290]
NIH3T3 IC50
6.03 μM
Compound: PFL
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 24 hrs by MTT assay
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 24 hrs by MTT assay
[PMID: 30389290]
NIH3T3 IC50
6.09 μM
Compound: PFL
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 30389290]
Vero IC50
5.01 μM
Compound: Penfluridol
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
10.1101/2020.03.20.999730
Vero CC50
8.77 μM
Compound: Penfluridol
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
10.1101/2020.03.20.999730
體外研究
(In Vitro)

Penfluridol (R-16341；1.25-40 μM；24、48 小時) 會降低攜帶 FLT3-WT 或 FLT3-ITD 突變的人 AML 細(xì)胞的細(xì)胞活力[2]。
Penfluridol (7.5 μM；24 小時) 會導(dǎo)致攜帶 FLT3-WT 和 FLT3-ITD 突變的 AML 細(xì)胞凋亡[2]。
Penfluridol (1.25-7.5 μM；24 小時) 通過觸發(fā) LC3 周轉(zhuǎn)和酸性泡狀細(xì)胞器 (AVO) 形成來誘導(dǎo) ROS 介導(dǎo)的自噬[2]。
Penfluridol (1μM；2 小時) 抑制 TNFα 誘導(dǎo)的 ERK，JNK 和 P38 的磷酸化水平[3]。
Penfluridol (1μM；2 小時) 抑制 TNFα 誘導(dǎo)的 IL-1β，IL-6，IL-17 和 NOS2 的 mRNA 表達(dá)[3]。
Penfluridol 抑制脾臟幼稚的 CD4+T 細(xì)胞對 Th1 和 Th17 的分化，并抑制 M1 巨噬細(xì)胞極化[3]。

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

Cell Viability Assay[2]

Cell Line: Human AML cell lines, HL-60 (FLT3-WT), U937 (FLT3-WT), and MV4–11 (FLT3-ITD)
Concentration: 1.25, 2.5, 5, 10, 20, 40 μM
Incubation Time: 24, 48 h
Result: Significantly reduced cell viability in a concentration-dependent manner.

Apoptosis Analysis[2]

Cell Line: HL-60 and U937 cells harboring FLT3-WT
Concentration: 7.5?μM
Incubation Time: 24?h
Result: Induced concentration-dependent increases in the sub-G1 population.
Triggered caspase-3 activation and corresponding PARP-1 cleavage in concentration- and time-dependent manners.

Cell Autophagy Assay[2]

Cell Line: U937 and HL-60 cells
Concentration: 1.25, 2.5, 5, 7.5 μM
Incubation Time: 24?h
Result: 5 μM and 7.5?μM respectively induced dominant LC3B-II formation and caspase-3 activation in U937 and HL-60 cells.

Western Blot Analysis[3]

Cell Line: BMDMs
Concentration: 1 μM
Incubation Time: Pretream for 2 h
Result: Obviously inhibited the increased phosphorylation levels of ERK, JNK, and p38 by TNFα (10 ng/mL; 15, 30, 60 min).

RT-PCR[3]

Cell Line: BMDMs
Concentration: 1 μM
Incubation Time: Pretream for 2 h
Result: Inhibited TNFα-induced mRNA expressions of IL-1β, IL-6, IL-17, and NOS2.
體內(nèi)研究
(In Vivo)

Penfluridol (10 mg/kg；每日灌胃給藥；從第一次免疫后的第18天開始) 顯著降低了膠原蛋白誘導(dǎo)的關(guān)節(jié)炎的嚴(yán)重程度[3]。

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

Animal Model: DBA/1J male mice aged 10–12 weeks with type II chicken collagen-induced arthritis (CIA) model[3]
Dosage: 10 mg/kg
Administration: Daily oral gavage; from the 18th day after the first immunization
Result: Inhibited inflammatory cell infiltration, suppressed pannus formation, and protected articular cartilage from damage.
obviously decreased mRNA expressions of CXCL10 and MCP-1 in inflamed joints and statistically reduced production levels of inflammatory cytokines IL-1β and IL-6 in sera.
分子量

523.97

Formula

C28H27ClF5NO
CAS 號
性狀

固體

顏色

White to off-white

中文名稱

五氟利多
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : ≥ 100 mg/mL (190.85 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.9085 mL 9.5425 mL 19.0851 mL
5 mM 0.3817 mL 1.9085 mL 3.8170 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請?jiān)?年內(nèi)使用， -20°C儲存時，請?jiān)?個月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實(shí)驗(yàn)：

請根據(jù)您的 實(shí)驗(yàn)動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.77 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.77 mM); 懸濁液; 超聲助溶

    此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動物溶解方案計(jì)算器
請輸入動物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.93%

參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請?jiān)?年內(nèi)使用， -20°C儲存時，請?jiān)?個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9085 mL 9.5425 mL 19.0851 mL 47.7127 mL
5 mM 0.3817 mL 1.9085 mL 3.8170 mL 9.5425 mL
10 mM 0.1909 mL 0.9543 mL 1.9085 mL 4.7713 mL
15 mM 0.1272 mL 0.6362 mL 1.2723 mL 3.1808 mL
20 mM 0.0954 mL 0.4771 mL 0.9543 mL 2.3856 mL
25 mM 0.0763 mL 0.3817 mL 0.7634 mL 1.9085 mL
30 mM 0.0636 mL 0.3181 mL 0.6362 mL 1.5904 mL
40 mM 0.0477 mL 0.2386 mL 0.4771 mL 1.1928 mL
50 mM 0.0382 mL 0.1909 mL 0.3817 mL 0.9543 mL
60 mM 0.0318 mL 0.1590 mL 0.3181 mL 0.7952 mL
80 mM 0.0239 mL 0.1193 mL 0.2386 mL 0.5964 mL
100 mM 0.0191 mL 0.0954 mL 0.1909 mL 0.4771 mL
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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產(chǎn)品名稱：
Penfluridol
目錄號：
HY-B1077
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