喷他脒
| 中文名称 | 喷他脒 |
|---|---|
| 中文同义词 | 4,4'-(戊烷-1,5-二基双(氧基))二苯脒;喷他脒;4,4'-二脒基二苯氧基戊烷;喷他脒碱;羟乙磺胺戊烷脒;4,4'-(戊烷-1,5-二基双(氧基))二苯甲脒;4,4'-(戊烷-1,5-二基双(氧基))二苯甲脒 |
| 英文名称 | Pentamidine |
| 英文同义词 | 4,4’-(pentamethylenedioxy)dibenzamidine;4,4’-diamidino-alpha,omega-diphenoxypentane;4,4’-diamidinodiphenoxypentane;p,p’-(pentamethylene-dioxy)bis-benzamidine;p,p’-(pentamethylenedioxy)dibenzamidine;4,4'-[1,5-PENTANEDIYLBIS(OXY)]BIS-BENZENECARBOXIMIDAMIDE;PENTAMIDINE;4,4’-(1,5-pentanediylbis(oxy))bis-benzenecarboximidamid |
| CAS号 | 100-33-4 |
| 分子式 | C19H24N4O2 |
| 分子量 | 340.42 |
| EINECS号 | 202-841-0 |
| 相关类别 | 黑热病药;化合物;原料药;抑制剂;医药原料药;Intermediates & Fine Chemicals;Pharmaceuticals;Amines;Aromatics;NEBUPENT;其他原料;抗寄生虫 |
| Mol文件 | 100-33-4.mol |
| 结构式 |  |
喷他脒 性质
| 熔点 | 186 °C (dec.) |
|---|---|
| 沸点 | 476.22°C (rough estimate) |
| 密度 | 1.1805 (rough estimate) |
| 折射率 | 1.6620 (estimate) |
| 储存条件 | Sealed in dry,Store in freezer, under -20°C |
| 溶解度 | 可溶于DMSO、甲醇（少量） |
| 形态 | 固体 |
| 酸度系数(pKa) | pKa 11.4 (Uncertain) |
| 颜色 | 白色至类白色 |
IC50: 2.5 μM (
Leishmania infantum
)
Protein tyrosine phosphatases (PTPases)
Phosphatase of regenerating liver (PRL)
Pentamidine (0-10 µg/mL; 6 days; WM9, DU145, C4-2, Hey, WM480, and A549 cells) treatment inhibits the growth of cancer cells in a concentration-dependent manner.
The cytotoxic properties of Pentamidine isethionate towards the promastigotes of the protozoan parasite
Leishmania infantum
is determined. The leishmanicidal activity of Pentamidine isethionate is 60 times higher after 72 h of incubation than that of Cisplatin. Pentamidine isethionate induces a higher amount of programmed cell death (PCD) than Cisplatin, which is associated with inhibition of DNA synthesis and cell-cycle arrest in the G2/M phase. Binding of Pentamidine isethionate to calf-thymus DNA (CT-DNA) induces conformational changes in the DNA double helix, consistent with a B-->A transition. The interaction of Pentamidine isethionate with ubiquitin leads to a 6% increase in the beta-sheet content of the protein.
Cell Viability Assay
| Cell Line: | WM9, DU145, C4-2, Hey, WM480, and A549 cells |
| Concentration: | 0-10 µg/mL |
| Incubation Time: | 6 days |
| Result: | The growth of all six of the cell lines in culture was inhibited in a concentration-dependent manner with complete growth inhibition of the cell lines occurring at 10 µg/mL. |
Pentamidine (0.25 mg/mouse; intramuscular injection; every 2 days; for 4 weeks; athymic nude mice) treatment markedly inhibits the growth of WM9 human melanoma tumors in nude mice.
| Animal Model: | Athymic nude mice (6 weeks old) injected with WM9 cells |
| Dosage: | 0.25 mg/mouse |
| Administration: | Intramuscular injection; every 2 days; for 4 weeks |
| Result: | Markedly inhibited the growth of WM9 human melanoma tumors in nude mice. |
安全信息
| 危险品运输编号 | 3249 |
|---|---|
| 危险等级 | 6.1(b) |
| 包装类别 | III |
| 毒害物质数据 | 100-33-4(Hazardous Substances Data) |