O-(氯乙酰氨甲酰基)烟曲霉素醇

中文名称:

O-(氯乙酰氨甲酰基)烟曲霉素醇

中文同义词:

TNP 470/O-(氯乙酰氨甲酰基)烟曲霉素醇;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;甲硫氨酸氨肽酶-2抑制剂(TNP-470);夫马菌素醇

英文名称:

AGM-1470

英文同义词:

NSC642492;O-(chloroacetylcarbamoyl)fumagillol;O-(CHLOROACETYLCARBAMOYL)FUMAGILLOLTNP-470 AGM-1470;[(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;AGM-1470;Carbamic acid, (chloroacetyl)-, (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;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

CAS号:

129298-91-5

分子式:

C19H28ClNO6

分子量:

401.88

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

129298-91-5.mol

比旋光度 

D24 -46.6° (c = 0.44 in CHCl3)

密度 

1.26±0.1 g/cm3(Predicted)

储存条件 

-20°C

溶解度 

DMSO: >15mg/mL

形态

White to light yellow solid

酸度系数(pKa)

7.19±0.46(Predicted)

生物活性

TNP-470 是甲硫氨酸氨肽酶-2 抑制剂，也是一种血管生成抑制剂。

靶点

methionine aminopeptidase-2, angiogenesis

体外研究

No significant difference of apoptotic cell numbers is observed between cells treated with TNP-470 and the controls. The IC 50 s 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.

体内研究

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.

危险品标志 

Xi

危险类别码 

36/37/38

安全说明 

26

WGK Germany 

2