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  3. Afzelin

Afzelin  (Synonyms: Kaempferol-3-O-rhamnoside)

目錄號(hào): HY-N1441 純度: 99.62%
COA 產(chǎn)品使用指南 技術(shù)支持

Afzelin (Kaempferol-3-O-rhamnoside) 是黃酮醇糖苷,具有抗炎、抗氧化應(yīng)激反應(yīng)、抗細(xì)胞凋亡、抗心臟細(xì)胞毒性的作用。Afzelin 可減弱線粒體損傷,增強(qiáng)線粒體生物合成,降低線粒體相關(guān)蛋白,Parkin 和 PTEN 誘導(dǎo)的假定激酶 1 (putative kinase 1) 的水平。Afzelin 可提高 D-半乳糖胺 (GalN)/LPS 處理的小鼠的存活率,預(yù)防阿霉素 (HY-15142A) 誘導(dǎo)的心臟毒性和東莨菪堿 (HY-N0296) 誘導(dǎo)的神經(jīng)損傷。Afzelin 還抑制卵清蛋白引發(fā)的哮喘和過敏。

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)

Afzelin Chemical Structure

Afzelin Chemical Structure

CAS No. : 482-39-3

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10 mM * 1 mL in Ethanol ¥1210
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1 mg ¥500
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Other Forms of Afzelin:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Afzelin (Kaempferol-3-O-rhamnoside)It is a flavonol glycoside that has anti-inflammatory, anti-oxidative stress response, anti-apoptotic, and anti-cardiac cytotoxic effects. AfzelinIt can reduce mitochondrial damage, enhance mitochondrial biosynthesis, and reduce mitochondria-related proteins. Parkinand PTENinduced putative kinase 1 (putative kinase 1)s level. AfzelinCan be improved D-galactosamine(GalN)/LPSSurvival rate of mice treated with doxorubicin prophylaxis (HY-15142A)Induced cardiotoxicity and scopolamine (HY-N0296)-induced neurological injury. AfzelinAlso inhibits asthma and allergies caused by ovalbumin[1][2][3][4].

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
BMDC IC50
> 50 μM
Compound: 18
Inhibition of LPS-induced IL-12 p40 production in wild-type C57BL/6 mouse BMDC pretreated with compound for 1 hr before LPS treatment measured 16 hrs by ELISA
Inhibition of LPS-induced IL-12 p40 production in wild-type C57BL/6 mouse BMDC pretreated with compound for 1 hr before LPS treatment measured 16 hrs by ELISA
[PMID: 25769817]
BMDC IC50
> 50 μM
Compound: 18
Inhibition of LPS-induced IL-6 production in wild-type C57BL/6 mouse BMDC pretreated with compound for 1 hr before LPS treatment measured 16 hrs by ELISA
Inhibition of LPS-induced IL-6 production in wild-type C57BL/6 mouse BMDC pretreated with compound for 1 hr before LPS treatment measured 16 hrs by ELISA
[PMID: 25769817]
BMDC IC50
> 50 μM
Compound: 18
Inhibition of LPS-induced TNF-alpha production in wild-type C57BL/6 mouse BMDC pretreated with compound for 1 hr before LPS treatment measured 16 hrs by ELISA
Inhibition of LPS-induced TNF-alpha production in wild-type C57BL/6 mouse BMDC pretreated with compound for 1 hr before LPS treatment measured 16 hrs by ELISA
[PMID: 25769817]
體外研究
(In Vitro)

Afzelin (20-80 μM; 12 h) 可保護(hù)心肌細(xì)胞 H9C2 細(xì)胞的活力,抵抗 DOX(1 μM;12 小時(shí))誘導(dǎo)的毒性[2]。
Afzelin 的抗心臟毒性作用會(huì)被 AMPKα 抑制劑 Dorsomorphin 消除[2]。

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

Cell Viability Assay[2]

Cell Line: Cardiomyocyte H9C2 cells
Concentration: 20, 40, and 80 μM
Incubation Time: 12 h, 24 h
Result: Was safe and non-toxic to H9C2 cells even under 80 μM concentration.
Reversed the effect of DOX, sunch that decreased the cell survival rate, and elevated apoptotic rate, as well as induced the oxidative stress and mitochondrial dysfunction in H9C2 cells.
體內(nèi)研究
(In Vivo)

Afzelin (5, 10 mg/kg/day; 口服; 共 20 天) 可以濃度依賴的方式減輕 DOX 毒性導(dǎo)致的心臟損傷。其通過上調(diào) p-AMP 激活蛋白激酶 α (AMPKα) 和 Sirtuin1 (SIRT1) 水平而發(fā)揮心臟保護(hù)作用[2]。
Afzelin (0.1-10 mg/kg/day; 口服; 共 5 天) 可下調(diào)哮喘小鼠模型中的 GATA 結(jié)合蛋白 3 轉(zhuǎn)錄因子 (GATA3) 來減輕哮喘表型。Afzelin 抑制 GATA3 而減少 Th2 細(xì)胞因子,GATA3 是 Th2 細(xì)胞因子分化和產(chǎn)生的主要調(diào)節(jié)因子[3]。
Afzelin(100 ng/μL; 腦室注射; 每周 3 次, 共 1 個(gè)月)可改善服用東莨菪堿 (HY-N0296) 的小鼠的突觸可塑性和認(rèn)知/記憶行為[4]

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

Animal Model: C57BL/6 Mouse[2]
Dosage: 5 mg/kg/day, 10 mg/kg/day
Administration: Oral gavage for 20 days, while C57BL/6 mouse were treated with 4 mg/kg/d (ip, injected at day 1, 7, 14) DXO for 3 doses.
Result: Attenuated DOX-induced cardiac damage and reduced serum levels of alanine aminotransferase and pro-inflammatory cytokines.
Also upregulated the expression of p-AMP-activated protein kinase α (AMPKα) and Sirtuin1 (SIRT1).
Animal Model: Asthma murine model sensitized by ovalbumin (OVA)[3]
Dosage: 0.1, 1 and 10 mg/kg
Administration: PO; once daily from day 19 to day 23
Result: Suppressed eosinophil infiltration, allergic airway inflammation, airway hyperresponsiveness, OVA-specific IgE and Th2 cytokine secretion.
Animal Model: Scopolamine induced mouse model[4]
Dosage: 100 ng/μL
Administration: ICV, administered into the third ventricle of the hypothalamus; 3 time per week for 1 month
Result: Resulted the restoration of the cholinergic systems and molecular signal transduction via CREB-BDNF pathways.
Led to improved neurocognitive and neuroprotective effects on synaptic plasticity and behaviors partly through the increase in CREB-BDNF signaling.
分子量

432.38

Formula

C21H20O10

CAS 號(hào)
性狀

固體

顏色

Light yellow to yellow

中文名稱

阿福豆甙

結(jié)構(gòu)分類
初始來源
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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(shí)驗(yàn): 

DMSO 中的溶解度 : 116.67 mg/mL (269.83 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)使用新開封的 DMSO)

Ethanol 中的溶解度 : 12.5 mg/mL (28.91 mM; 超聲助溶)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.3128 mL 11.5639 mL 23.1278 mL
5 mM 0.4626 mL 2.3128 mL 4.6256 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, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)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(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(qǐng)依序添加每種溶劑: 10% EtOH    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.78 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 EtOH 儲(chǔ)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(qǐng)依序添加每種溶劑: 10% EtOH    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.78 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 EtOH 儲(chǔ)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(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 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(chǔ)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(chǔ)備液濃度超過該產(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: 99.62%

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, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)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
Ethanol / DMSO 1 mM 2.3128 mL 11.5639 mL 23.1278 mL 57.8195 mL
5 mM 0.4626 mL 2.3128 mL 4.6256 mL 11.5639 mL
10 mM 0.2313 mL 1.1564 mL 2.3128 mL 5.7820 mL
15 mM 0.1542 mL 0.7709 mL 1.5419 mL 3.8546 mL
20 mM 0.1156 mL 0.5782 mL 1.1564 mL 2.8910 mL
25 mM 0.0925 mL 0.4626 mL 0.9251 mL 2.3128 mL
DMSO 30 mM 0.0771 mL 0.3855 mL 0.7709 mL 1.9273 mL
40 mM 0.0578 mL 0.2891 mL 0.5782 mL 1.4455 mL
50 mM 0.0463 mL 0.2313 mL 0.4626 mL 1.1564 mL
60 mM 0.0385 mL 0.1927 mL 0.3855 mL 0.9637 mL
80 mM 0.0289 mL 0.1445 mL 0.2891 mL 0.7227 mL
100 mM 0.0231 mL 0.1156 mL 0.2313 mL 0.5782 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:
Afzelin
目錄號(hào):
HY-N1441
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