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471-95-4

中文名稱(chēng) 蟾毒它靈
英文名稱(chēng) 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 2025/04/03 15:11:06
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(duì)照品
Γ-日蟾毒配質(zhì)
蟾毒它靈(標(biāo)準(zhǔn)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(lèi)別
化學(xué)試劑:其他酯類(lèi)化合物

物理化學(xué)性質(zhì)

外觀性狀無(wú)色液體,可溶于甲醇、乙醇、DMSO等有機(jī)溶劑,來(lái)源于石菖蒲,薔薇科植物枇杷葉。
熔點(diǎn)223°C (rough estimate)
比旋光度D20 +5.4° (c = 0.5 in chloroform)
沸點(diǎn)474.53°C (rough estimate)
密度1.0942 (rough estimate)
折射率1.4593 (estimate)
儲(chǔ)存條件-20°C儲(chǔ)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(lèi)白色固體
顏色White to off-white
CAS 數(shù)據(jù)庫(kù)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(xiǎn)品運(yùn)輸編號(hào)3172
危險(xiǎn)等級(jí)6.1(a)
包裝類(lèi)別II
海關(guān)編碼29329990

常見(jiàn)問(wèn)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(kāi)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(duì)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(lèi)固醇內(nèi)酯,具有強(qiáng)大的抗腫瘤活性。Bufotalin 誘導(dǎo)癌細(xì)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.
蟾毒它靈價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱(chēng)CAS號(hào)包裝價(jià)格
2025/02/08HY-N0878蟾毒它靈
Bufotalin
471-95-41 mg411元
2025/02/08HY-N0878蟾毒它靈
Bufotalin
471-95-45mg900元
2025/02/08HY-N0878蟾毒它靈
Bufotalin
471-95-410mM * 1mLin DMSO990元
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