蟾毒它靈
| 中文名稱 | 蟾毒它靈 |
|---|---|
| 中文同義詞 | 蟾毒它靈;Γ-日蟾毒配質(zhì);蟾蜍皂素;蟾毒他靈;蟾蜍他靈;蟾蜍皂素,蟾蜍他靈,蟾毒他靈;蟾毒它靈(蟾蜍皂素,蟾蜍他靈,蟾毒他靈);蟾毒它靈, 蟾蜍他靈 |
| 英文名稱 | Bufotaline |
| 英文同義詞 | 3-BETA-14,16-BETA-TRIHYDROXY-5BETA-BUFA-20,22-DIENOLIDE SULFATE;16-(Acetyloxy)-3,14-dihydroxybufa-20,22-dienolide;22-dienolide,3-beta,14,16-beta-trihydroxy-5-beta-bufa-216-acetate;5beta-Bufa-20,22-dienolide, 3beta,14,16beta-trihydroxy-, 16-acetate;Bufa-20,22-dienolide, 16-(acetyloxy)-3,14-dihydroxy-, (3beta,5beta,16beta)-;Bufotaline;BUFOTALIN;BUFOTALIN SULFATE |
| CAS號(hào) | 471-95-4 |
| 分子式 | C26H36O6 |
| 分子量 | 444.56 |
| EINECS號(hào) | |
| 相關(guān)類別 | 中藥對(duì)照品;標(biāo)準(zhǔn)品;植物提取物;中草藥成分;對(duì)照品;標(biāo)準(zhǔn)品-對(duì)照品;標(biāo)準(zhǔn)品 -中藥標(biāo)準(zhǔn)品;其它萜類;分析試劑-對(duì)照品;Miscellaneous Natural Products;20版藥典新增;標(biāo)準(zhǔn)品，對(duì)照品 |
| Mol文件 | 471-95-4.mol |
| 結(jié)構(gòu)式 |  |
蟾毒它靈 性質(zhì)
| 熔點(diǎn) | 223°C (rough estimate) |
|---|---|
| 沸點(diǎn) | 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) |
| 儲(chǔ)存條件 | Store at -20°C |
| 溶解度 | DMF：30mg/mL； DMSO：30mg/mL；乙醇：30mg/mL |
| 形態(tài) | 白色至類白色固體。 |
| 酸度系數(shù)(pKa) | 14.44±0.70(Predicted) |
| 顏色 | 白色至米白色 |
| CAS 數(shù)據(jù)庫(kù) | 471-95-4 |
| NIST化學(xué)物質(zhì)信息 | Bufotalin(471-95-4) |
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. |
安全信息
| 危險(xiǎn)品運(yùn)輸編號(hào) | 3172 |
|---|---|
| 危險(xiǎn)等級(jí) | 6.1(a) |
| 包裝類別 | II |
| 海關(guān)編碼 | 29329990 |
| 更新日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
|---|---|---|---|---|---|
| 2024/11/08 | HY-N0878 | Bufotalin | 1 mg | 411元 | |
| 2024/11/08 | HY-N0878 | 蟾毒它靈 Bufotalin | 471-95-4 | 5mg | 900元 |