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1094250-15-3

中文名稱 恩格林A
英文名稱 Englerin A
CAS 1094250-15-3
分子式 C26H34O6
分子量 442.54
MOL 文件 1094250-15-3.mol
1094250-15-3 結(jié)構(gòu)式 1094250-15-3 結(jié)構(gòu)式

基本信息

中文別名
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
英文別名
Englerin A
(?)-Englerin A
(-)-ENGLERIN A
Englerin A high purity
(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
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)-

物理化學(xué)性質(zhì)

沸點(diǎn)550.3±50.0 °C(Predicted)
密度1.20±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
酸度系數(shù)(pKa)12.88±0.10(Predicted)
形態(tài)Solid
顏色White to light yellow

常見問題列表

生物活性
Englerin A 是一種有效和選擇性的 TRPC4 和 TRPC5 通道的活化劑,EC50 值分別為 11.2 和 7.6 nM。Englerin A 通過增加 Ca2+ 內(nèi)流和 Ca2+ 細(xì)胞超負(fù)荷來誘導(dǎo)腎癌細(xì)胞死亡。
靶點(diǎn)

hTRPC4

11.2 nM (EC 50 )

hTRPC5

7.6 nM (EC 50 )

體外研究

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.

體內(nèi)研究

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

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