蟾毒它灵
- CAS号:471-95-4
- 英文名:Bufotaline
- 中文名:蟾毒它灵
- CBNumber:CB0313399
- 分子式:C26H36O6
- 分子量:444.56
- MOL File:471-95-4.mol
- 熔点 :223°C (rough estimate)
- 沸点 :474.53°C (rough estimate)
- 比旋光度 :D20 +5.4° (c = 0.5 in chloroform)
- 密度 :1.0942 (rough estimate)
- 折射率 :1.4593 (estimate)
- 储存条件 :Store at -20°C
- 溶解度 :DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml
- 形态 :White to off-white solid.
- 酸度系数(pKa) :14.44±0.70(Predicted)
- 颜色 :White to off-white
- CAS 数据库 :471-95-4
- NIST化学物质信息 :Bufotalin(471-95-4)
- 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
蟾毒它灵性质、用途与生产工艺
- 产品描述 蟾毒它灵是蟾酥中的主要化合物之一。众多的研究发现蟾毒它灵具有良好的抗肿瘤活性，具有很大的药物应用开发前景。目前含有蟾毒它灵的口服液、片剂已应用于临床，对肝癌、肺癌、胃癌等具有较好的疗效。
- 生物活性 Bufotalin 是一种从 Venenum Bufonis 分离的类固醇内酯，具有强大的抗肿瘤活性。Bufotalin 诱导癌细胞凋亡 (apoptosis)，也诱导内质网应激激活。
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体外研究
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. -
体内研究
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. - 化学性质 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。
- 用途 橙花叔醇具有抗炎，行咳的作用。
- 用途 用于含量测定/鉴定/药理实验等
- 类别 有毒物品
- 毒性分级 剧毒
- 急性毒性 皮下-小鼠 LD50: 0.4 毫克/公斤; 静脉-小鼠 LD50: 4.13 毫克/公斤
- 可燃性危险特性 热分解排出有毒辛辣刺激烟雾
- 储运特性 库房通风低温干燥
- 灭火剂 水,干粉、干砂、二氧化碳、泡沫、1211灭火剂
- 更新日期：2024/11/08
- 产品编号：HY-N0878
- 产品名称：Bufotalin
- CAS编号：
- 包装：1 mg
- 价格：411元
- 更新日期：2024/11/08
- 产品编号：HY-N0878
- 产品名称：蟾毒它灵 Bufotalin
- CAS编号：471-95-4
- 包装：5mg
- 价格：900元
- 公司名称：Apin Chemicals Limited (UK)
- 联系电话：--
- 电子邮件：info@apinchemicals.com
- 国家：英国
- 产品数：6184
- 优势度：60
- 公司名称：Leancare Ltd.
- 联系电话：--
- 电子邮件：enquiry@leancare.co.uk
- 国家：英国
- 产品数：6446
- 优势度：42
- 公司名称：APIN-NP
- 联系电话：--
- 电子邮件：info@apinchemicals.com
- 国家：英国
- 产品数：6807
- 优势度：42
