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5610-40-2

中文名稱 一葉秋堿
英文名稱 SECURININE
CAS 5610-40-2
分子式 C13H15NO2
分子量 217.26
MOL 文件 5610-40-2.mol
更新日期 2024/12/23 13:11:55
5610-40-2 結(jié)構(gòu)式 5610-40-2 結(jié)構(gòu)式

基本信息

中文別名
葉秋堿
一葉堿
葉底珠堿
一葉萩堿
一葉秋堿
硝酸一葉秋堿
一葉萩堿、一葉秋堿
一葉秋堿 ,一葉萩堿
SECURININE 一葉萩堿
一葉秋堿 ,一葉萩堿(標(biāo)準(zhǔn)品)
英文別名
securinin
SECURININE
Securan one
(-)-securinin
SECURAN-11-ONE
SECURININE(RG)
Securinan-11-on
securinan-11-one
(2β,7S,9S)-Securinan-11-one
1,2,3,4,10,10a-Hexahydro-10-hydroxy-
所屬類別
原料藥:中樞興奮藥

物理化學(xué)性質(zhì)

外觀性狀黃色結(jié)晶粉末,可溶于甲醇、乙醇、DMSO等有機(jī)溶劑,來源于大戟科植物葉底珠的嫩枝葉或根,葉下珠。
熔點140-1420C
比旋光度D20 -1042° (c = 1 in alc)
沸點357.82°C (rough estimate)
密度1.30±0.1 g/cm3 (20 ºC 760 Torr)
折射率1.5300 (estimate)
儲存條件-20°C冷凍
溶解度二甲基亞砜:≥25mg/mL
酸度系數(shù)(pKa)8.29±0.20(Predicted)
形態(tài)粉末
顏色黃色
旋光性 (optical activity)[α]/D -980 to -1015 (C=1, MeOH)

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS06
警示詞危險
危險性描述H301
危險品標(biāo)志T,Xn
危險類別碼23/24/25-22
安全說明36/37/39-45
WGK Germany3
RTECS號VS4115000

應(yīng)用領(lǐng)域

用途1
中樞神經(jīng)系統(tǒng)興奮藥。
用途2
抗菌活性;對中樞神經(jīng)系統(tǒng)有興奮作用;抗腫瘤作用

常見問題列表

生物活性
(-)-Securinine 是一種植物來源的生物堿,也是一種 GABAA 受體拮抗劑。
靶點
TargetValue
GABA receptor
()
體外研究

(-)-Securinine is a major plant-derived alkaloid and also a GABA A receptor antagonist. (-)-Securinine is significantly potent on HeLa cells growth inhibition with IC 50 values of 7.02±0.52 μg/mL (32.3 μM). (-)-Securinine induces apoptosis in a dose-dependent manner in the tested cells, increases the percentage of ROS positive cells and depolarized cells as well as stimulates the activity of ERK1/2, caspase-9 and -3/7. (-)-Securinine also induces cell cycle arrest in S phase. Real-time PCR analysis shows high expression of tumor necrosis factor receptor superfamily (TNFRSF) genes in the cells stimulated with (-)-Securinine.

體內(nèi)研究

In this tumor model, tumor growth is significantly impaired with (-)-Securinine treatment indicating that (-)-Securinine has potential as an Acute Myeloid Leukemia (AML) therapeutic. (-)-Securinine treated mice (n=5 mice, bilateral tumors), exhibit an average of more than 75% smaller tumors than vehicle treated mice at the end of the study period.

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