戊烷脒
| 中文名稱 | 戊烷脒 |
|---|---|
| 中文同義詞 | 戊烷脒;4,4'-[1,5-戊烷二基二(氧基)]二苯甲脒]二鹽酸鹽;噴他脒二鹽酸鹽;噴他脒二鹽酸鹽,10 MM DMSO 溶液 |
| 英文名稱 | PentaMidine-d4 2HCl |
| 英文同義詞 | PentaMidine-d4 2HCl;PentaMidine (dihydrochloride);4,4'-[1,5-Pentanediylbis(oxy)]bisbenzenecarboximidamide] dihydrochloride;Benzenecarboximidamide, 4,4'-[1,5-pentanediylbis(oxy)]bis-, dihydrochloride (9CI);MP601205 dihydrochloride;MP601205 DIHYDROCHLORIDE;PENTAMIDINE;PTP1B,Pneumocystis,Parasite,Antibiotic,antitumor,Pentamidine,MP 601205,Inhibitor,Kidney,MP-601205,carinii,Bacterial,cell-cycle,pneumonia,MP601205,Phosphatase,inhibit,DNA,Pentamidine dihydrochloride,biosynthetics,Fungal,arrest;Pentamidine dihydrochloride, 10 mM in DMSO |
| CAS號(hào) | 50357-45-4 |
| 分子式 | C19H26Cl2N4O2 |
| 分子量 | 413.34134 |
| EINECS號(hào) | |
| 相關(guān)類別 | 小分子抑制劑，天然產(chǎn)物;Inhibitors |
| Mol文件 | 50357-45-4.mol |
| 結(jié)構(gòu)式 |  |
戊烷脒 性質(zhì)
| 熔點(diǎn) | 232-234° |
|---|---|
| 儲(chǔ)存條件 | Store at -20°C |
| 溶解度 | 溶于 DMSO > 10 mM |
| 形態(tài) | 粉末 |
戊烷脒在體外有殺利什曼原蟲(chóng)作用，在體內(nèi)效果不如五價(jià)銻劑。其殺原蟲(chóng)原理可能系干擾敏感原蟲(chóng)的糖酵解?？诜改c道吸收差，肌注吸收完全，并很快分布于各組織，血藥濃度維持時(shí)間短暫，但在肝、腎組織中保留時(shí)間可達(dá)數(shù)日?？赏ㄟ^(guò)胎盤，但不進(jìn)乳汁。 戊烷脒用于銻劑治療無(wú)效及不宜用銻劑治療的黑熱病的患者、對(duì)銻劑過(guò)敏者或治療中有粒細(xì)胞減少者。
不良反應(yīng)大，如胃部灼感、惡心、嘔吐、頭痛、頭昏、腹痛、心悸等。偶見(jiàn)皮膚瘙癢、黃疸、氣促、血壓下降等，也可引起低血糖或高血糖。在治療早期有發(fā)熱和脾臟增大等。由于刺激作用注射部位出現(xiàn)硬結(jié)與血腫。
1.因可使原有的肺結(jié)核病灶惡化，故肺結(jié)核患者禁用。
2.本品水溶液不穩(wěn)定，臨用時(shí)應(yīng)新鮮配制，并注意避光。肌注前可用滅菌注射用水配成4%～10%溶液。
3.劑量增至每次5～6mg/kg，14～16日為一療程，治愈率可提高。
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
| 毒性 | LD50 in mice (mg/g): 0.028 i.v.; 0.064 s.c. (Wein) |
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