471-95-4
基本信息
蟾蜍他灵
蟾毒他灵
蟾蜍皂素
蟾毒它灵对照品
Γ-日蟾毒配质
蟾毒它灵(标准品)
蟾毒它灵, 蟾蜍他灵
蟾蜍皂素,蟾蜍他灵,蟾毒他灵
蟾蜍皂素、蟾蜍他灵、蟾毒他灵、日蟾毒配质
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
物理化学性质
| 外观性状 | 无色液体，可溶于甲醇、乙醇、DMSO等有机溶剂，来源于石菖蒲，蔷薇科植物枇杷叶。 |
| 熔点 | 223°C (rough estimate) |
| 比旋光度 | D20 +5.4° (c = 0.5 in chloroform) |
| 沸点 | 474.53°C (rough estimate) |
| 密度 | 1.0942 (rough estimate) |
| 折射率 | 1.4593 (estimate) |
| 储存条件 | -20°C储存 |
| 溶解度 | DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml |
| 酸度系数(pKa) | 14.44±0.70(Predicted) |
| 形态 | 白色至类白色固体 |
| CAS 数据库 | 471-95-4 |
| NIST化学物质信息 | Bufotalin(471-95-4) |
应用领域
安全数据
| 危险品运输编号 | 3172 |
| 危险等级 | 6.1(a) |
| 包装类别 | II |
| 海关编码 | 29329990 |
常见问题列表
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. |
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. |