TNP-470|129298-91-5|(夫马菌素醇 ; AGM-1470)-陌孚医药/Medlife

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TNP-470 (Synonyms: 夫马菌素醇 ; AGM-1470)

目录号: PC15761 纯度: ≥98%

CAS No. :129298-91-5

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中文名称	TNP-470
中文别名	O-(氯乙酰氨甲酰基)烟曲霉素醇;[(3R,4S,5S,6R)-5-甲氧基-4-[(2R,3R)-2-甲基-3-(3-甲基丁-2-烯基)环氧乙烷-2-基]-1-氧杂螺[2.5]辛烷-6-醇] N-(2-氯乙酰基)氨基甲酸酯;TNP 470/O-(氯乙酰氨甲酰基)烟曲霉素醇
英文名称	TNP-470
英文别名	AGM-1470;O-(Chloroacetylcarbamoyl)fumagillol;[(3R,4S,5S,6R)-5-Methoxy-4-[(2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl]-1-oxaspiro[2.5]octan-6-yl] N-(2-chloroacetyl)carbamate;TNP 470,N-(2-Chloroacetyl)carbamicacid(3R,4S,5S,6R)-5-Methoxy-4-[(2R,3R)-2-methyl-3-(3-methyl-2-buten-1-yl)-2-oxiranyl]-1-oxaspiro[2.5]oct-6-ylester;TNP-470;6-O-chloroacetylcarbamoylfumagillol;NSC642492;O-Chloracetyl-carbamoyl fumagillol;O-(chloroacetyl-carbaMoyl) fuMagillol,TNP-470;O-(CHLOROACETYLCARBAMOYL)FUMAGILLOLTNP-470 AGM-1470;(Chloracetyl) carbamic acid (3R,4S,5S,6R)-5-methoxy-4-[(2R,3R)-2-methyl-3-(3-methyl-2-butenyl)oxiranyl]-1-oxaspiro[2.5]oct-6-yl ester;TNP 470;(3R,4S,5S,6R)-5-Methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl)-1-oxaspiro[2;DSSTox_CID_21141;DSSTox_RID_79634;DSSTox_GSID_41141;Tox21_303433;(3R,4S,5S,6R)-5-methoxy-4-[(3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl]-1-oxaspiro[2.5]oct-6-yl (chloroacetyl)carbamate
Cas No.	129298-91-5
分子式	C₁₉H₂₈ClNO₆
分子量	401.88
包装储存	-20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

生物活性

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

性状

Solid

IC50 & Target[1][2]

methionine aminopeptidase-2, angiogenesis

体外研究(In Vitro)

No significant difference of apoptotic cell numbers is observed between cells treated with TNP-470 and the controls. The IC₅₀s of TNP-470 are 16.86±0.9 μg/mL, 3.16±0.6 μg/mL and 1.78±0.8 μg/mL for KKU-M213 cells at 24, 48 and 72 h, respectively. The results show that TNP-470 significantly reduces the number of migrated cells and invaded cells as compare with the vehicle treated group. TNP-470 decreases the migrated cells of KKU-M213 to 26% and of KKU-M214 to 11% (P<0.01). Similarly, TNP-470 also significantly affects cell invasion, the number of invaded cells is reduced to 25% in KKU-M213 (P<0.01) and to 15% in KKU-M214 (P<0.01). The relative expressions of MMP2, MMP9 and c-MYC in TNP-470 treated cells are significantly suppressed compare to the vehicle treated cells.

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

体内研究(In Vivo)

Treatment with TNP-470 attenuates (P<0.05) liver lipid accumulation compare to high fat fed (HFF) mice. By day 5, TNP-470 treated mice consume significantly less grams of high fat food than vehicle treated HFF mice. By day 15 of treatment, TNP-470 mice are consuming an equivalent number of calories to that of chow fed mice, despite the provision of high fat diet. Treatment with TNP-470 increases (P<0.05) expression of adipose tissue LPL mRNA, compare to chow-fed and high-fat fed controls. TNP-470 decreases energy intake and increases energy expenditure.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

-20°C, stored under nitrogen

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

ClinicalTrial

参考文献

[1]. Kidoikhammouan S, et al. TNP-470, a methionine aminopeptidase-2 inhibitor, inhibits cell proliferation, migration and invasion of human cholangiocarcinoma cells 体外研究. Asian Pac J Cancer Prev. 2012;13 Suppl:155-60. [Information]

[2]. White HM, et al. The angiogenic inhibitor TNP-470 decreases caloric intake and weight gain in high-fat fed mice. Obesity (Silver Spring). 2012 Oct;20(10):2003-9. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (248.83 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	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
10 mM	0.2488 mL	1.2442 mL	2.4883 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.22 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.22 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
2.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.22 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.22 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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