恩格林A

中文名称:

恩格林A

中文同义词:

恩格林A;(1S,2R,5R,6R,7S,8R,10R)-10-(GLYCOLOYLOXY)-8-ISOPROPYL-1,5-DIMETHYL-11-OXATRICYCLO[6.2.1.02,6]UNDEC-7-YL (2E)-3-PHENYLACRYLATE

英文名称:

Englerin A

英文同义词:

Englerin A;Englerin A high purity;(-)-ENGLERIN A;2-Propenoic acid, 3-phenyl-, (1R,3aR,4S,5R,7R,8S,8aR)-decahydro-5-[(2-hydroxyacetyl)oxy]-1,4-dimethyl-7-(1-methylethyl)-4,7-epoxyazulen-8-yl ester, (2E)-;(?)-Englerin A;(1S,2R,5R,6R,7S,8R,10R)-10-(Glycoloyloxy)-8-isopropyl-1,5-dimethyl-11-oxatricyclo[6.2.1.02,6]undec-7-yl(2E)-3-phenylacrylate

CAS号:

1094250-15-3

分子式:

C26H34O6

分子量:

442.54

EINECS号:

相关类别:

中药对照品

Mol文件:

1094250-15-3.mol

生物活性

Englerin A 是一种有效和选择性的 TRPC4 和 TRPC5 通道的活化剂，EC50 值分别为 11.2 和 7.6 nM。Englerin A 通过增加 Ca2+ 内流和 Ca2+ 细胞超负荷来诱导肾癌细胞死亡。

靶点

hTRPC4 11.2 nM (EC 50 ) hTRPC5 7.6 nM (EC 50 )

hTRPC4 11.2 nM (EC 50 )

hTRPC5 7.6 nM (EC 50 )

体外研究

Englerin A (0.15-2500 nM; 48 h) characteristic concentration-dependent suppresses cells growth of the A-498 cells treated with the control siRNA while has little effect on the growth of cells treated with TRPC4 siRNAs. Englerin A (0.001nM-10 μM; 48 h) inhibits cells viability in HEK293T cells overexpressing TRPC5. Englerin A (3 nM; 1-240 s) evokes sustained elevation of the intracellular Ca 2+ concentration within 1 min in HEK 293 cells over-expressing human TRPC4. Englerin A (0.1-1000 nM; 1-300 s) evokes intracellular Ca 2+ elevations in A498 cells as well with an EC 50 of 10 nM.

体内研究

Englerin A (5 mg/kg; i.p daily except Sunday) markedly inhibits tumor growth during the 2-week treatment period in mice.