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471-95-4

中文名稱 蟾毒它靈
英文名稱 Bufotaline
CAS 471-95-4
分子式 C26H36O6
分子量 444.56
MOL 文件 471-95-4.mol
更新日期 2025/01/24 10:07:28
471-95-4 結(jié)構(gòu)式 471-95-4 結(jié)構(gòu)式

基本信息

中文別名
蟾毒它靈
蟾蜍他靈
蟾毒他靈
蟾蜍皂素
蟾毒它靈對照品
Γ-日蟾毒配質(zhì)
蟾毒它靈(標準品)
蟾毒它靈, 蟾蜍他靈
蟾蜍皂素,蟾蜍他靈,蟾毒他靈
蟾蜍皂素、蟾蜍他靈、蟾毒他靈、日蟾毒配質(zhì)
英文別名
BUFOTALIN
Bufotaline
BUFOTALIN(SH)
Bufotalin std.
GAMMA-BUFOTALIN
Bufotaline ,98%
BUFOTALIN SULFATE
Bufotalin Standard
Bufotaline cas no. 471-95-4
16-(Acetyloxy)-3,14-dihydroxybufa-20,22-dienolide
所屬類別
化學(xué)試劑:其他酯類化合物

物理化學(xué)性質(zhì)

外觀性狀無色液體,可溶于甲醇、乙醇、DMSO等有機溶劑,來源于石菖蒲,薔薇科植物枇杷葉。
熔點223°C (rough estimate)
比旋光度D20 +5.4° (c = 0.5 in chloroform)
沸點474.53°C (rough estimate)
密度1.0942 (rough estimate)
折射率1.4593 (estimate)
儲存條件-20°C儲存
溶解度DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml
酸度系數(shù)(pKa)14.44±0.70(Predicted)
形態(tài)白色至類白色固體
顏色White to off-white
CAS 數(shù)據(jù)庫471-95-4
NIST化學(xué)物質(zhì)信息Bufotalin(471-95-4)

應(yīng)用領(lǐng)域

用途1
橙花叔醇具有抗炎,行咳的作用。

安全數(shù)據(jù)

危險品運輸編號3172
危險等級6.1(a)
包裝類別II
海關(guān)編碼29329990

常見問題列表

產(chǎn)品描述
蟾毒它靈是蟾酥中的主要化合物之一。眾多的研究發(fā)現(xiàn)蟾毒它靈具有良好的抗腫瘤活性,具有很大的藥物應(yīng)用開發(fā)前景。目前含有蟾毒它靈的口服液、片劑已應(yīng)用于臨床,對肝癌、肺癌、胃癌等具有較好的療效。
生物活性
Bufotalin 是一種從 Venenum Bufonis 分離的類固醇內(nèi)酯,具有強大的抗腫瘤活性。Bufotalin 誘導(dǎo)癌細胞凋亡 (apoptosis),也誘導(dǎo)內(nèi)質(zhì)網(wǎng)應(yīng)激激活。
體外研究

Bufotalin (0.1-2.5 μM; 12-96 hours) treatment dose- and time-dependently inhibits MG-63 osteoblastoma cell survival.
Bufotalin (0.5-2.5 μM; 48 hours) treatment dose-dependently increases the percentage of Annexin V positive cells (apoptotic cells) and caspase-12 activity in MG-63 cells. Bufotalin-induced osteoblastoma cell apoptosis is associated with caspase-12 activation.
Bufotalin (0.5-2.5 μM; 12 hours) treatment dose-dependently induces C/EBP homologous protein (CHOP) expression as well as PERK and IRE1 phosphorylation in MG-63 cells. Bufotalin induces endoplasmic reticulum (ER) stress activation in cells.
Bufotalin treatment induces cell cycle arrest at G2/M phase through down-regulation of Aurora A, CDC25, CDK1, cyclin A and cyclin B1, as well as up-regulation of p53 and p21 in HepG2 cells. Bufotalin treatment also induces apoptosis which was accompanied by decrease in mitochondrial membrane potential, increases in intracellular calcium level and reactive oxygen species production, activations of caspase-9 and -3, cleavage of poly ADP-ribose polymerase (PARP) as well as changes in the expressions of bcl-2 and bax.

Cell Viability Assay

Cell Line: MG-63 osteoblastoma cells
Concentration: 0.1 μM, 0.5 μM, 1 μM, 2.5 μM
Incubation Time: 12 hours, 24 hours, 48 hours, 72 hours, 96 hours
Result: Inhibited MG-63 osteoblastoma cell survival.

Apoptosis Analysis

Cell Line: MG-63 cells
Concentration: 0.5 μM, 1 μM, 2.5 μM
Incubation Time: 48 hours
Result: Dose-dependently increased the percentage of Annexin V positive cells (apoptotic cells) and caspase-12 activity in MG-63 cells.

Western Blot Analysis

Cell Line: MG-63 cells
Concentration: 0.5 μM, 1 μM, 2.5 μM
Incubation Time: 12 hours
Result: Dose-dependently induced CHOP expression as well as PERK and IRE1 phosphorylation in MG-63 cells.
體內(nèi)研究

Bufotalin (0.5-1 mg/kg; intraperitoneal injection; twice daily; for 7 days) treatment shows a significantly reduced tumor growth in mice.

Animal Model: SCID male mice (4-6 weeks old) injected with U2OS cells
Dosage: 0.5 mg/kg, 1 mg/kg
Administration: Intraperitoneal injection; twice daily; for 7 days
Result: Inhibited U2OS osteoblastoma cell growth in mice.
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