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  1. Apoptosis Autophagy
  2. Apoptosis Autophagy
  3. Acacetin

Acacetin  (Synonyms: 金合歡素; 5,7-Dihydroxy-4'-methoxyflavone)

目錄號(hào): HY-N0451 純度: 99.83%
COA 產(chǎn)品使用指南

Acacetin (5,7-Dihydroxy-4'-methoxyflavone) 是一種口服有效的類黃酮,來(lái)自 Dendranthema morifolium。Acacetin 停在 PI3Kγ 的 ATP 結(jié)合口袋中。Acacetin 導(dǎo)致癌細(xì)胞周期停滯,并誘導(dǎo)細(xì)胞凋亡和自噬。Acacetin 具有有效的抗癌和抗炎活性,有用于疼痛相關(guān)疾病研究的潛力。

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(gè)人用途提供產(chǎn)品和服務(wù)

Acacetin Chemical Structure

Acacetin Chemical Structure

CAS No. : 480-44-4

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1 mg ¥165
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5 mg ¥330
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10 mg ¥495
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25 mg ¥850
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50 mg ¥1275
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100 mg ¥1912
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500 mg ¥4113
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Other Forms of Acacetin:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an orally active flavonoid derived from Dendranthema morifolium. Acacetin docks in the ATP binding pocket of PI3Kγ. Acacetin causes cell cycle arrest and induces apoptosis and autophagy in cancer cells. Acacetin has potent anti-cancer and anti-inflammatory activity and has the potential for pain-related diseases research[1][2].

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.4 μg/mL
Compound: Acacetin
Cytotoxicity against human A549 cells by SRB assay
Cytotoxicity against human A549 cells by SRB assay
[PMID: 31784199]
HCT-15 IC50
0.4 μg/mL
Compound: Acacetin
Cytotoxicity against human HCT15 cells by SRB assay
Cytotoxicity against human HCT15 cells by SRB assay
[PMID: 31784199]
MOLM-13 IC50
9.1 μM
Compound: 28
Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 33393294]
Monocyte IC50
22 μM
Compound: Acacetin
Inhibition of TNFalpha expression in LPS-stimulated human monocytes treated 30 mins before LPS challenge measured after 14 hrs by ELISA
Inhibition of TNFalpha expression in LPS-stimulated human monocytes treated 30 mins before LPS challenge measured after 14 hrs by ELISA
[PMID: 10096854]
MV4-11 IC50
6.8 μM
Compound: 28
Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 33393294]
Neutrophil IC50
7 μM
Compound: 4d
Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of superoxide anion radical-induced lucigenin oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay
Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of superoxide anion radical-induced lucigenin oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay
[PMID: 23871908]
RAW264.7 IC50
27.7 μM
Compound: 27
Inhibition of LPS-stimulated nitric oxide production in mouse RAW264.7 cells by Greiss method
Inhibition of LPS-stimulated nitric oxide production in mouse RAW264.7 cells by Greiss method
[PMID: 27955927]
RAW264.7 IC50
5.9 μM
Compound: 17
Inhibition of LPS induced NO production in mouse RAW264.7 cells measured after 24 hrs by Griess reagent based assay
Inhibition of LPS induced NO production in mouse RAW264.7 cells measured after 24 hrs by Griess reagent based assay
[PMID: 33667099]
RAW264.7 IC50
53.7 μM
Compound: 27
Inhibition of LPS/INF-gamma-stimulated nitric oxide production in mouse RAW264.7 cells by Greiss method
Inhibition of LPS/INF-gamma-stimulated nitric oxide production in mouse RAW264.7 cells by Greiss method
[PMID: 27955927]
RAW264.7 IC50
6.2 μM
Compound: 11
Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
[PMID: 31747281]
RAW264.7 CC50
60.9 μM
Compound: 17
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 33667099]
SK-MEL-2 IC50
0.4 μg/mL
Compound: Acacetin
Cytotoxicity against human SK-MEL-2 cells by SRB assay
Cytotoxicity against human SK-MEL-2 cells by SRB assay
[PMID: 31784199]
SK-OV-3 IC50
0.4 μg/mL
Compound: Acacetin
Cytotoxicity against human SKOV3 cells by SRB assay
Cytotoxicity against human SKOV3 cells by SRB assay
[PMID: 31784199]
XF498 IC50
0.4 μg/mL
Compound: Acacetin
Cytotoxicity against human XF498 cells by SRB assay
Cytotoxicity against human XF498 cells by SRB assay
[PMID: 31784199]
體外研究
(In Vitro)

Acacetin (5,7-Dihydroxy-4'-methoxyflavone; 10-200 μM; 24 hours) decreases cell viabilities in a dose-dependent manner. Acacetin has little effect on human normal glial cell line HEB and non-tumorigenic epithelial cell line MCF-10A[1].
Acacetin (50-150 μM; 24 hours) causes G2/M cell cycle arrest and induces apoptosis and autophagy[1].
Acacetin (50-150 μM; 24 hours) leads to decreases in levels of PI3Kγ-p110, p-AKT, p-mTOR, p-p70S6K, and p-ULK in a dose-dependent manner[1].

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

Cell Viability Assay[1]

Cell Line: Breast cancer MCF-7 cells, hepatocellular carcinoma SMMC-7721 cells, lung adenocarcinoma A549 cells, esophageal carcinoma Eca109 cells
Concentration: 10, 20, 40, 60, 80, 100, 150, 200 μM
Incubation Time: 24 hours
Result: Decreased cancer cell viabilities in a dose-dependent manner.
Had IC50 values of 82.75?μM, 103.9 μM, 157.4 μM, 54.7 μM in MDA-MB-231, MCF-7, A549, Eca109 cells, respectively.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 50, 100, 150 μM
Incubation Time: 24 hours
Result: Resulted in increase in percentage of cells at G2/M phase and decrease in percentage of cells at G1 and S phase in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 50, 100, 150 μM
Incubation Time: 24 hours
Result: Induced apoptosis.

Cell Autophagy Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 50, 100, 150 μM
Incubation Time: 24 hours
Result: Induced autophagy.
Resulted in marked increases in EGFP-LC3 puncta formation and a dose-dependent accumulation of LC3-II.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 50, 100, 150 μM
Incubation Time: 24 hours
Result: Resulted in decrease in levels of Bcl-2 and Bcl-xL and increase in levels of p53.
Led to decreases in levels of PI3Kγ-p110, p-AKT, p-mTOR, p-p70S6K, and p-ULK in a dose-dependent manner.
Had little or no effect on expression of PI3Kα, PI3Kβ, PI3Kδ, p-ERK, p-p38, and p-JNK.
體內(nèi)研究
(In Vivo)

Acacetin (5,7-Dihydroxy-4'-methoxyflavone; 5, 20 mg/kg/day; orally; for 3 days) significantly suppresses microglial activation in an LPS-induced neuroinflammation mouse model[2].
Acacetin (25 mg/kg/day; orally; for 3 days) reduces neuronal cell death in an animal model of ischemia[2].
Acacetin (1.8-56.2 mg/kg/day; ip; single dose) decreases visceral and inflammatory nociception and prevented the formalin-induced oedema[3].

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

Animal Model: Male C57BL/6 mice, 7 weeks of age[2]
Dosage: 5, 20 mg/kg
Administration: Orally; once a day for 3 days
Result: Significantly suppressed microglial activation in an LPS-induced (ip; 5mg/kg) neuroinflammation mouse model.
分子量

284.26

Formula

C16H12O5

CAS 號(hào)
性狀

固體

顏色

Light yellow to yellow

中文名稱

金合歡素;刺槐黃素

結(jié)構(gòu)分類
初始來(lái)源
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 125 mg/mL (439.74 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 3.5179 mL 17.5895 mL 35.1791 mL
5 mM 0.7036 mL 3.5179 mL 7.0358 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(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(dòng)物實(shí)驗(yàn):

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)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(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)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(chǔ)備液可以根據(jù)儲(chǔ)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (7.32 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL(飽和度未知)的澄清溶液,此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

    1 mL 工作液為例,取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中,混合均勻。

以下溶解方案,請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶。

  • 方案 一

    請(qǐng)依序添加每種溶劑: 50% PEG300    50% Saline

    Solubility: 5 mg/mL (17.59 mM); 懸濁液; 超聲助溶

  • 方案 二

    請(qǐng)依序添加每種溶劑: 0.5% CMC-Na/saline water

    Solubility: 10 mg/mL (35.18 mM); 懸濁液; 超聲助溶

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動(dòng)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(guò) 2%。
方案所需 助溶劑 包括:DMSO ,均可在 MCE 網(wǎng)站選購(gòu)。 ,Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)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(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)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(guò)半月以上,請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)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: 99.83%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(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 3.5179 mL 17.5895 mL 35.1791 mL 87.9477 mL
5 mM 0.7036 mL 3.5179 mL 7.0358 mL 17.5895 mL
10 mM 0.3518 mL 1.7590 mL 3.5179 mL 8.7948 mL
15 mM 0.2345 mL 1.1726 mL 2.3453 mL 5.8632 mL
20 mM 0.1759 mL 0.8795 mL 1.7590 mL 4.3974 mL
25 mM 0.1407 mL 0.7036 mL 1.4072 mL 3.5179 mL
30 mM 0.1173 mL 0.5863 mL 1.1726 mL 2.9316 mL
40 mM 0.0879 mL 0.4397 mL 0.8795 mL 2.1987 mL
50 mM 0.0704 mL 0.3518 mL 0.7036 mL 1.7590 mL
60 mM 0.0586 mL 0.2932 mL 0.5863 mL 1.4658 mL
80 mM 0.0440 mL 0.2199 mL 0.4397 mL 1.0993 mL
100 mM 0.0352 mL 0.1759 mL 0.3518 mL 0.8795 mL
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  • 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:
Acacetin
目錄號(hào):
HY-N0451
需求量: