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  1. Apoptosis Autophagy Anti-infection Metabolic Enzyme/Protease
  2. Apoptosis Autophagy Bacterial Endogenous Metabolite
  3. Isoalantolactone

Isoalantolactone  (Synonyms: 異土木香內(nèi)酯; (+)-Isoalantolactone; Isohelenin)

目錄號: HY-N0780 純度: 99.99%
COA 產(chǎn)品使用指南 技術(shù)支持

Isoalantolactone 是一種烷化劑,用作細(xì)胞凋亡 (apoptosis) 誘導(dǎo)劑。

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)

Isoalantolactone Chemical Structure

Isoalantolactone Chemical Structure

CAS No. : 470-17-7

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10 mM * 1 mL in DMSO ¥496
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Customer Review

Other Forms of Isoalantolactone:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Isoalantolactone is an apoptosis inducer, which also acts as an alkylating agent.

IC50 & Target

Apoptosis[1]

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.38 μg/mL
Compound: 8
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
[PMID: 23451797]
HeLa IC50
8.15 μM
Compound: Isoalantolactone
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay
[PMID: 31784199]
HepG2 IC50
1.77 μg/mL
Compound: 8
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
[PMID: 23451797]
HT-1080 IC50
0.795 μg/mL
Compound: 8
Antiproliferative activity against human HT1080 cells assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
Antiproliferative activity against human HT1080 cells assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
[PMID: 23451797]
HUVEC IC50
2.5 μg/mL
Compound: 8
Antiproliferative activity against human HUVEC assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
Antiproliferative activity against human HUVEC assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
[PMID: 23451797]
Platelet IC50
> 516.5 μM
Compound: Isoalantolactone
Antimigraine activity in bovine citreated platelet assessed as inhibition of [14C]serotonin release after 6 mins by scintillation counting
Antimigraine activity in bovine citreated platelet assessed as inhibition of [14C]serotonin release after 6 mins by scintillation counting
[PMID: 1431933]
體外研究
(In Vitro)

Isoalantolactone 對 K562 人白血病細(xì)胞系具有良好的細(xì)胞毒性 (IC50=1.2 μM)[1]。使用 PANC-1、BxPC3 和 HPAC 細(xì)胞系評估 Isoalantolactone 對胰腺癌的細(xì)胞毒性作用。用 Isoalantolactone 處理 24 小時(shí)以劑量依賴性方式抑制 PANC-1 細(xì)胞生長。在 80 μM 時(shí)抑制率超過 90%,達(dá)到 50% 生長抑制的濃度 (IC50) 為 40 μM。在 Isoalantolactone 處理的 BxPC3 和 HPAC 細(xì)胞中觀察到類似的細(xì)胞活力喪失趨勢,IC50 值分別為 43 和 48 μM。用 3 mM N-乙酰半胱氨酸 (NAC)? (一種特定的 ROS 清除劑) 預(yù)處理可恢復(fù)細(xì)胞的活力,這表明 Isoalantolactone 通過 ROS 的產(chǎn)生對細(xì)胞活力發(fā)揮細(xì)胞毒性作用[2]。

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

體內(nèi)研究
(In Vivo)

與對照組相比,Isoalantolactone 對 CD1 小鼠的急性和慢性毒性作用通過測量體重、血液生化和肝腎組織病理學(xué)的變化來評估。小鼠對異胡桃內(nèi)酯具有良好的耐受性,并且在兩個(gè)實(shí)驗(yàn)期間 (7 天和 30 天) 期間,在 100 mg/kg 的劑量下未發(fā)現(xiàn)死亡率或任何藥毒性跡象。在兩個(gè)實(shí)驗(yàn)期間,對照和處理小鼠的體重增加和食物消耗是可比較的,并且組織病理學(xué)和血液生化參數(shù)沒有藥物相關(guān)的變化。使用蘇木精和伊紅染色評估肝臟和腎臟的組織病理學(xué)變化,并與肝腎功能生物標(biāo)志物相關(guān)聯(lián)。對照組和處理組肝腎結(jié)構(gòu)未見明顯形態(tài)學(xué)改變。給藥第7天處理組血清谷丙轉(zhuǎn)氨酶 (ALT) 和天冬氨酸轉(zhuǎn)氨酶 (AST) 水平略有升高,但與對照組無顯著差異 (P<0.05)。在給藥第 7 天,處理組總膽紅素 (TBIL) 濃度顯著增加 (1.43±0.26 vs 對照組 0.76±0.12,P<0.05)。同樣,腎功能生物標(biāo)志物的變化也沒有顯著差異 (P<0.05) ) 在劑量第 7 天時(shí)對照組和處理組的血清中。肌酐 (Cr) 的濃度略有增加,而處理組的血尿素氮 (BUN) 的濃度略有降低。給小鼠注射異胡桃內(nèi)酯100 mg/kg 30天,血清AST、ALT、TBIL和BUN水平略有下降[2]。

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

分子量

232.32

Formula

C15H20O2

CAS 號
性狀

固體

顏色

White to off-white

中文名稱

異土木香內(nèi)酯;異阿蘭內(nèi)酯

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
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 : 100 mg/mL (430.44 mM; 超聲助溶; 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 4.3044 mL 21.5220 mL 43.0441 mL
5 mM 0.8609 mL 4.3044 mL 8.6088 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, 2 years; -20°C, 1 year。-80°C儲存時(shí),請?jiān)?年內(nèi)使用, -20°C儲存時(shí),請?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 (10.76 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (10.76 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 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

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: 99.99%

參考文獻(xiàn)
Cell Assay
[2]

Cell viability is assessed by MTT assay. Briefly PANC-1, BxPC3, and HPAC cells are treated with DMSO or Isoalantolactone (5, 10, 20, 40, 80 and 100 μM) in the presence or absence of 3 mM NAC for 24 h. Following treatment, the MTT reagent is added (500 μg/mL) and cells are further incubated at 37°C for 4 h. Subsequently 150 μL DMSO is added to dissolve farmazan crystals and absorbance is measured at 570 nm in a microplate reader. The percentage of cell viability is calculated[2].

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

Animal Administration
[2]

Mice[2]
In vivo studies for acute and chronic toxicity are conducted on 10-12 week old CD1 mice weighing 27-30 g. The mice are maintained in a specific pathogen-free grade animal facility on a 12-h light/dark cycles at 25±2°C. Mice are randomly divided into four groups. Group A (n=4) administered with 50 μL DMSO intraperitonially for 7 days; Group B (n=4) administered with Isoalantolactone (100 mg/kg body weight) in 50 μL DMSO intraperitonially for 7 days; Group C (n=4) administered with 50 μL DMSO for 30 days and Group D (n=4) administered with Isoalantolactone (100 mg/kg body weight) in 50 μL DMSO intraperitonially for 30 days. At the first and last day of the experiments, the body weight of each mouse is measured. At the end of experiments (at dose day 7 for acute toxicity & dose day 30 for chronic toxicity), mice are anesthetized using Pentobarbital sodium (50 mg/kg ip), blood is collected via cardiac puncture, allowed to clot for 10 min and centrifuge at 1000×g for 10 min at room temperature. Serum is separated and stored at -20°C until analysis. The liver and kidneys are excised and processed for hematoxylin and eosin staining followed established procedures.

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

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, 2 years; -20°C, 1 year。-80°C儲存時(shí),請?jiān)?年內(nèi)使用, -20°C儲存時(shí),請?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 4.3044 mL 21.5220 mL 43.0441 mL 107.6102 mL
5 mM 0.8609 mL 4.3044 mL 8.6088 mL 21.5220 mL
10 mM 0.4304 mL 2.1522 mL 4.3044 mL 10.7610 mL
15 mM 0.2870 mL 1.4348 mL 2.8696 mL 7.1740 mL
20 mM 0.2152 mL 1.0761 mL 2.1522 mL 5.3805 mL
25 mM 0.1722 mL 0.8609 mL 1.7218 mL 4.3044 mL
30 mM 0.1435 mL 0.7174 mL 1.4348 mL 3.5870 mL
40 mM 0.1076 mL 0.5381 mL 1.0761 mL 2.6903 mL
50 mM 0.0861 mL 0.4304 mL 0.8609 mL 2.1522 mL
60 mM 0.0717 mL 0.3587 mL 0.7174 mL 1.7935 mL
80 mM 0.0538 mL 0.2690 mL 0.5381 mL 1.3451 mL
100 mM 0.0430 mL 0.2152 mL 0.4304 mL 1.0761 mL
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產(chǎn)品名稱:
Isoalantolactone
目錄號:
HY-N0780
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