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100-33-4

中文名稱 噴他脒
英文名稱 Pentamidine
CAS 100-33-4
分子式 C19H24N4O2
分子量 340.42
MOL 文件 100-33-4.mol
更新日期 2024/12/18 10:44:13
100-33-4 結(jié)構(gòu)式 100-33-4 結(jié)構(gòu)式

基本信息

中文別名
噴他脒
4,4'-二脒基二苯氧基戊烷
4,4'-(戊烷-1,5-二基雙(氧基))二苯脒
英文別名
NSC 9921
MP 601205
PENTAMIDINE
4,4’-diamidinodiphenoxypentane
4,4’-(pentamethylenedioxy)di-benzamidin
p,p’-(pentamethylenedioxy)dibenzamidine
4,4’-(pentamethylenedioxy)dibenzamidine
4,4'-(1,5-Pentanediylbisoxy)dibenzamidine
p,p’-(pentamethylene-dioxy)bis-benzamidine
4-[5-(4-amidinophenoxy)pentoxy]benzamidine
所屬類別
原料藥:抗絲蟲病及抗利什曼原蟲病藥

物理化學(xué)性質(zhì)

熔點186 °C (dec.)
沸點476.22°C (rough estimate)
密度1.1805 (rough estimate)
折射率1.6620 (estimate)
儲存條件-20°C Freezer, Under Inert Atmosphere
溶解度可溶于DMSO、甲醇(少量)
酸度系數(shù)(pKa)pKa 11.4 (Uncertain)
形態(tài)固體
顏色白色至灰白色

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H315-H302-H335-H319
危險品運輸編號3249
危險等級6.1(b)
包裝類別III
毒害物質(zhì)數(shù)據(jù)100-33-4(Hazardous Substances Data)

圖譜信息

常見問題列表

生物活性
Pentamidine (MP-601205) 是一種抗微生物劑,會干擾 DNA 的生物合成。Pentamidine 抑制寄生蟲 Leishmania infantum,IC50 為 2.5 μM。Pentamidine 是一種有效的選擇性蛋白酪氨酸磷酸酶 (PTPases) 和再生肝磷酸酶 (PRL) 抑制劑。Pentamidine 可用于岡比亞錐蟲病,抗銻利什曼病和卡氏肺孢子蟲肺炎的研究??鼓[瘤活性,抗菌活性。
靶點

IC50: 2.5 μM ( Leishmania infantum )
Protein tyrosine phosphatases (PTPases)
Phosphatase of regenerating liver (PRL)

體外研究

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.
體內(nèi)研究

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.
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