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  1. Metabolic Enzyme/Protease
  2. Aminopeptidase
  3. TNP-470

TNP-470  (Synonyms: 夫馬菌素醇 ; AGM-1470)

目錄號(hào): HY-101932 純度: 99.87%
COA 產(chǎn)品使用指南

TNP-470 是甲硫氨酸氨肽酶-2 抑制劑,也是一種血管生成抑制劑。

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)

TNP-470 Chemical Structure

TNP-470 Chemical Structure

CAS No. : 129298-91-5

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥1547
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1 mg ¥880
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5 mg ¥1750
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10 mg ¥2800
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100 mg   詢價(jià)  

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

  • 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

TNP-470 is a methionine aminopeptidase-2 inhibitor and also an angiogenesis inhibitor.

IC50 & Target

methionine aminopeptidase-2[1], angiogenesis[2]

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
50 μM
Compound: TNP470
Antiproliferative activity human A549 cells after 20 hrs by MTT assay
Antiproliferative activity human A549 cells after 20 hrs by MTT assay
[PMID: 20149494]
Bel-7402 IC50
≥ 50 μM
Compound: TNP470
Antiproliferative activity human Bel7402 cells after 20 hrs by MTT assay
Antiproliferative activity human Bel7402 cells after 20 hrs by MTT assay
[PMID: 20149494]
BGC-823 IC50
1.48 μM
Compound: TNP-470
Antiproliferative activity against human BGC823 cells after 24 hrs by MTT assay
Antiproliferative activity against human BGC823 cells after 24 hrs by MTT assay
[PMID: 21925884]
CPAE IC50
0.04 ng/mL
Compound: 7
Tested in vitro for its ability to inhibit cell proliferation of calf pulmonary artery endothelial cells measured calorimetrically by SRB method
Tested in vitro for its ability to inhibit cell proliferation of calf pulmonary artery endothelial cells measured calorimetrically by SRB method
[PMID: 10636239]
EL4 IC50
0.03 ng/mL
Compound: 7
Tested in vitro for its ability to inhibit cell proliferation of lymphoma EL-4 cells measured calorimetrically by MTT method
Tested in vitro for its ability to inhibit cell proliferation of lymphoma EL-4 cells measured calorimetrically by MTT method
[PMID: 10636239]
HeLa IC50
2.02 μM
Compound: TNP-470
Antiproliferative activity against human HeLa cells after 24 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 24 hrs by MTT assay
[PMID: 21925884]
HepG2 IC50
0.86 μM
Compound: TNP-470
Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay
[PMID: 21925884]
HUVEC IC50
0.0089 μM
Compound: TNP470
Antiproliferative activity HUVEC after 20 hrs by MTT assay
Antiproliferative activity HUVEC after 20 hrs by MTT assay
[PMID: 20149494]
HUVEC IC50
0.2 nM
Compound: 2a
Growth inhibition of HUVEC cells by XTT assay
Growth inhibition of HUVEC cells by XTT assay
[PMID: 17636946]
HUVEC IC50
0.5 μM
Compound: TNP-470
Antiangiogenic activity against HUVEC assessed as inhibition of VEGF-induced cell migration by NCI antiangiogenesis assay
Antiangiogenic activity against HUVEC assessed as inhibition of VEGF-induced cell migration by NCI antiangiogenesis assay
[PMID: 19084416]
HUVEC IC50
0.76 nM
Compound: TNP470
Antiproliferative activity against human HUVEC cells after 96 hrs by MTT assay
Antiproliferative activity against human HUVEC cells after 96 hrs by MTT assay
[PMID: 21296467]
HUVEC IC50
1 μM
Compound: TNP-470
Antiangiogenic activity against HUVEC assessed as inhibition of capillary-like structure formation by NCI antiangiogenesis assay
Antiangiogenic activity against HUVEC assessed as inhibition of capillary-like structure formation by NCI antiangiogenesis assay
[PMID: 19084416]
HUVEC IC50
1.96 μM
Compound: TNP-470
Antiproliferative against HUVEC after 48 hrs by MTT assay
Antiproliferative against HUVEC after 48 hrs by MTT assay
[PMID: 23582273]
HUVEC IC50
3.16 μM
Compound: TNP-470
Antiangiogenic activity against HUVEC assessed as growth inhibition by NCI antiangiogenesis assay
Antiangiogenic activity against HUVEC assessed as growth inhibition by NCI antiangiogenesis assay
[PMID: 19084416]
MCF7 IC50
≥ 50 μM
Compound: TNP470
Antiproliferative activity human MCF7 cells after 20 hrs by MTT assay
Antiproliferative activity human MCF7 cells after 20 hrs by MTT assay
[PMID: 20149494]
P388 IC50
> 10 ng/mL
Compound: 7
Tested in vitro for its ability to inhibit cell proliferation of murine leukemia P388D1 cells measured calorimetrically by MTT method
Tested in vitro for its ability to inhibit cell proliferation of murine leukemia P388D1 cells measured calorimetrically by MTT method
[PMID: 10636239]
SW 1116 IC50
5.54 μM
Compound: TNP-470
Antiproliferative activity against human SW1116 cells after 24 hrs by MTT assay
Antiproliferative activity against human SW1116 cells after 24 hrs by MTT assay
[PMID: 21925884]
體外研究
(In Vitro)

TNP-470 處理的細(xì)胞和對(duì)照之間沒(méi)有觀察到凋亡細(xì)胞數(shù)量的顯著差異。TNP-470 對(duì) KKU-M213 細(xì)胞 24、48 和 72 h 的 IC50 分別為 16.86±0.9 μg/mL、3.16±0.6 μg/mL 和 1.78±0.8 μg/mL .結(jié)果表明,與載體處理組相比,TNP-470 顯著減少了遷移細(xì)胞和侵入細(xì)胞的數(shù)量。TNP-470 將 KKU-M213 的遷移細(xì)胞減少至 26%,將 KKU-M214 的遷移細(xì)胞減少至 11% (P<0.01)。同樣,TNP-470 也顯著影響細(xì)胞侵襲,侵襲細(xì)胞數(shù)量在 KKU-M213 中降低至 25% (P<0.01),在 KKU-M214 中降低至 15% (P<0.01)。與載體處理的細(xì)胞相比,TNP-470 處理的細(xì)胞中 MMP2、MMP9c-MYC 的相對(duì)表達(dá)被顯著抑制[1]。

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

體內(nèi)研究
(In Vivo)

與高脂肪喂養(yǎng) (HFF) 小鼠相比,用 TNP-470 處理可減輕 (P<0.05) 肝臟脂質(zhì)積累。到第 5 天時(shí),TNP-470 處理的小鼠消耗的高脂肪食物克數(shù)明顯少于對(duì)照組的 HFF 小鼠。到處理的第 15 天,盡管提供高脂肪飲食,但 TNP-470 小鼠消耗的卡路里量與普通喂養(yǎng)小鼠的卡路里量相同。與食物喂養(yǎng)和高脂肪喂養(yǎng)的對(duì)照相比,用 TNP-470 處理會(huì)增加 (P<0.05) 脂肪組織 LPL mRNA 的表達(dá)。TNP-470 減少能量攝入并增加能量消耗[2]。

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

Clinical Trial
分子量

401.88

Formula

C19H28ClNO6

CAS 號(hào)
性狀

固液混合物

顏色

Colorless to off-white

中文名稱

夫馬菌素醇;夫馬吉欣

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 100 mg/mL (248.83 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)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.4883 mL 12.4415 mL 24.8830 mL
5 mM 0.4977 mL 2.4883 mL 4.9766 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 (stored under nitrogen)。-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(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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.22 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(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。
  • 方案 二

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

    Solubility: ≥ 2.5 mg/mL (6.22 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(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 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中,混合均勻。

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)。

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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: 99.87%

參考文獻(xiàn)
Cell Assay
[1]

MTT assays are applied to test cell viability. In brief, 3×103 cells per well are seeded in a 96-well plate and incubated with various concentration of TNP-470 for 24, 48, and 72 h at 37°C, 5% CO2. For comparison, cells cultured in the absence of TNP-470 are used as a control. After an incubation period, 10 μL MTT (0.5 mg/mL final concentration) is added to each well. After 4 h of additional incubation, 100 μL of 0.01 N HCl in isopropanol is added to dissolve the crystals. Absorption at 570 nm is determined by ELISA plate reader[1].

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

Animal Administration
[2]

Individually housed, 4 wk old male C57BL/6 mice are used in this study. After a 1 wk acclimation period, mice are randomly allocated to receive either standard chow diet or high-fat diet for 6.5 wk. Throughout the high-fat feeding period the mice are treated with TNP-470 at a dose of 20 mg/kg body weight, injected subcutaneously every other day (TNP; n=7) or a vehicle injection of an equivalent volume (HFF controls; n=7). Vehicle injections contain 3% ethanol in phosphate-buffered saline. Chow-fed control mice (chow; n=8) are sham injected. Mice are fed ad libitum with food replaced every 2 or 3 days. Body weights are collected three times per week. After 6.5 wk of feeding, animals are fasted for 16-h and sacrificed. Final body, liver, and epididymal adipose tissue weights are measured. Liver and adipose tissue samples are frozen in liquid nitrogen and stored at -80°C for subsequent analysis[2].

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

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 (stored under nitrogen)。-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
DMSO 1 mM 2.4883 mL 12.4415 mL 24.8830 mL 62.2076 mL
5 mM 0.4977 mL 2.4883 mL 4.9766 mL 12.4415 mL
10 mM 0.2488 mL 1.2442 mL 2.4883 mL 6.2208 mL
15 mM 0.1659 mL 0.8294 mL 1.6589 mL 4.1472 mL
20 mM 0.1244 mL 0.6221 mL 1.2442 mL 3.1104 mL
25 mM 0.0995 mL 0.4977 mL 0.9953 mL 2.4883 mL
30 mM 0.0829 mL 0.4147 mL 0.8294 mL 2.0736 mL
40 mM 0.0622 mL 0.3110 mL 0.6221 mL 1.5552 mL
50 mM 0.0498 mL 0.2488 mL 0.4977 mL 1.2442 mL
60 mM 0.0415 mL 0.2074 mL 0.4147 mL 1.0368 mL
80 mM 0.0311 mL 0.1555 mL 0.3110 mL 0.7776 mL
100 mM 0.0249 mL 0.1244 mL 0.2488 mL 0.6221 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:
TNP-470
目錄號(hào):
HY-101932
需求量: