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  1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Calcium Channel
  3. 3,5,7,3′,4′-Pentamethoxyflavone

3,5,7,3′,4′-Pentamethoxyflavone 

目錄號: HY-N7690 純度: 99.15%
COA 產(chǎn)品使用指南 技術(shù)支持

3,5,7,3’,4’-Pentamethoxyflavone 是一種 Ca2+ 通道 (Ca2+ channel) 抑制劑。3,5,7,3’,4’-Pentamethoxyflavone 可以保護(hù) DNA 免受氧化損傷。3,5,7,3’,4’-Pentamethoxyflavone 可通過鈣動員相關(guān)機(jī)制引起人類海綿體松弛。3,5,7,3’,4’-Pentamethoxyflavone 在中年雄性大鼠中可以促進(jìn)血管 eNOS 和胱硫氨酸-γ-裂解酶 CSE 蛋白的表達(dá),并調(diào)節(jié)血管功能。3,5,7,3’,4’-Pentamethoxyflavone 可用于糖尿病和心血管疾病的研究。

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3,5,7,3′,4′-Pentamethoxyflavone Chemical Structure

3,5,7,3′,4′-Pentamethoxyflavone Chemical Structure

CAS No. : 1247-97-8

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10 mM * 1 mL in DMSO ¥1229
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1 mg ¥650
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5 mg ¥1500
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10 mg ¥2400
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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

3,5,7,3’,4’-Pentamethoxyflavone is a Ca2+ channel inhibitor. 3,5,7,3’,4’-Pentamethoxyflavone can protect DNA from oxidative damage. 3,5,7,3’,4’-Pentamethoxyflavone can induce relaxation of the human corpus cavernosum through calcium mobilization-related mechanisms. 3,5,7,3’,4’-Pentamethoxyflavone can promote the expression of eNOS and cystathionine gamma lyase CSE proteins in middle-aged male rats and regulate vascular function. 3,5,7,3’,4’-Pentamethoxyflavone can be used in research related to diabetes and cardiovascular diseases[1][2][4].

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
2008 IC50
26.35 μM
Compound: 10
Inhibition of MRP1 (unknown origin) expressed in human 2008 cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay
Inhibition of MRP1 (unknown origin) expressed in human 2008 cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay
[PMID: 23851114]
A2780 ADR IC50
23.4 μM
Compound: 10
Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay
Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay
[PMID: 23851114]
L929 IC50
> 100 μM
Compound: 10
Cytotoxicity against mouse L929 cells after 5 days by MTS assay
Cytotoxicity against mouse L929 cells after 5 days by MTS assay
[PMID: 22743241]
MDA-MB-231 IC50
2.042 μM
Compound: 30
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
[PMID: 34971873]
MDCK-II IC50
0.822 μM
Compound: 10
Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of Hoechst 33342 preincubated for 30 mins before Hoechst 33342 addition measured after 120 mins by fluorescence assay
Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of Hoechst 33342 preincubated for 30 mins before Hoechst 33342 addition measured after 120 mins by fluorescence assay
[PMID: 23851114]
MDCK-II IC50
1.88 μM
Compound: 10
Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of pheophorbide-A preincubated for 30 mins before pheophorbide-A addition measured after 120 mins by flow cytometry
Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of pheophorbide-A preincubated for 30 mins before pheophorbide-A addition measured after 120 mins by flow cytometry
[PMID: 23851114]
體外研究
(In Vitro)

3,5,7,3’,4’-Pentamethoxyflavone (25-100 μg/mL) 可以保護(hù) pUC19 質(zhì)粒 DNA 免受氧化損傷[1]。
3,5,7,3’,4’-Pentamethoxyflavone (25-100 μg/mL) 可以減少小鼠外周血單核細(xì)胞的氧化 DNA 損傷[1]。
3,5,7,3’,4’-Pentamethoxyflavone 通過與電壓依賴性 Ca2+ 通道和鈣動員相關(guān)機(jī)制引起人類海綿體松弛[2]
3,5,7,3’,4’-Pentamethoxyflavone (100 μM, 48 h) 可以增加人腸道 Caco-2 細(xì)胞中腸道緊密連接 (TJ) 蛋白的表達(dá)并發(fā)揮體外腸道屏障促進(jìn)作用[3]。

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

Western Blot Analysis[3].

Cell Line: Human intestinal Caco-2 cells
Concentration: 100 μM
Incubation Time: 48 h
Result: Increased the cytoskeletal association of TJ proteins, such as ZO1, ZO2, occludin,claudin-1, claudin-3, and claudin-4, in the cells.
體內(nèi)研究
(In Vivo)

3,5,7,3’,4’-Pentamethoxyflavone (22 mg/kg; 每天 2 次; 6 周; 口服) 在中年雄性大鼠中可以促進(jìn)血管 eNOS 和胱硫氨酸-γ-裂解酶 CSE 蛋白的表達(dá),并通過對抗苯腎上腺素的收縮和增強(qiáng)乙酰膽堿的血管舒張來調(diào)節(jié)血管功能[4]。

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

Animal Model: Middle-aged (12–14 month old) Wistar male rats[4].
Dosage: 22 mg/kg
Administration: Oral gavage (p.o.); twice daily; 6 weeks
Result: Caused a decrease in plasma glucose and an increase in plasma HDL cholesterol levels of the rats.
分子量

372.37

Formula

C20H20O7

CAS 號
性狀

固體

顏色

White to light brown

結(jié)構(gòu)分類
初始來源
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數(shù)據(jù)
細(xì)胞實驗: 

DMSO 中的溶解度 : 25 mg/mL (67.14 mM; 超聲助溶 (<60°C); 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)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.6855 mL 13.4275 mL 26.8550 mL
5 mM 0.5371 mL 2.6855 mL 5.3710 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, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

動物實驗:

請根據(jù)您的 實驗動物和給藥方式 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:
——為保證實驗結(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)實驗的工作液,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 (6.71 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。

    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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.71 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,此方案實驗周期在半個月以上的動物實驗酌情使用。

    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玉米油中,混合均勻。

動物溶解方案計算器
請輸入動物實驗的基本信息:

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

由于實驗過程有損耗,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)。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,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。
動物實驗體內(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: 99.15%

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, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1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 2.6855 mL 13.4275 mL 26.8550 mL 67.1375 mL
5 mM 0.5371 mL 2.6855 mL 5.3710 mL 13.4275 mL
10 mM 0.2686 mL 1.3428 mL 2.6855 mL 6.7138 mL
15 mM 0.1790 mL 0.8952 mL 1.7903 mL 4.4758 mL
20 mM 0.1343 mL 0.6714 mL 1.3428 mL 3.3569 mL
25 mM 0.1074 mL 0.5371 mL 1.0742 mL 2.6855 mL
30 mM 0.0895 mL 0.4476 mL 0.8952 mL 2.2379 mL
40 mM 0.0671 mL 0.3357 mL 0.6714 mL 1.6784 mL
50 mM 0.0537 mL 0.2686 mL 0.5371 mL 1.3428 mL
60 mM 0.0448 mL 0.2238 mL 0.4476 mL 1.1190 mL
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產(chǎn)品名稱:
3,5,7,3′,4′-Pentamethoxyflavone
目錄號:
HY-N7690
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