喷他脒羟乙磺酸盐, Kinetoplast DNA 抑制剂

CAS: 140-64-7 货号: P408808 分子式: C19H24N4O2•2C2H6O4S 分子量: 592.68 EC号: 205-424-1 PubChem CID: 8813
有货
级别和纯度: 10mM in DMSO
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
P408808-1ml
现货 Stock Image
¥317.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述

异硫氰酸喷他脒盐已用于: 作为抗利什曼原虫、抗疟原虫和细胞毒性试验的阳性对照 作为原型化合物,分析抑制剂对人快速延迟性整流性相关基因 (HERG) K + 通道转运的影响 作为前鞭毛体中的抗利什曼原虫药物 卡氏肺囊虫抗菌药 。

Information

Pentamidine isethionate Pentamidine is an inhibitor of PRL Phosphatases and also inhibits synthesis of DNA, RNA and protein.
In vitro

Pentamidine is known experimentally to interfere with numerous cellular processes. Specifically, Pentamidine has been shown to bind to DNA in a nonintercalative manner and appears to preferentially bind to kinetoplast DNA in trypanosomes. Additionally, Pentamidine may inhibit RNA polymerase and ribosomal function, as well as nucleic acid, protein, phospholipid, and polyamine synthesis. Pentamidine also inhibits certain proteases, including trypsin, and impairs cellular oxygen consumption. Pentamidine has a potent in vitro antiprotozoal activity. Pentamidine displays cytotoxic activity against L. infantum promastigotes with IC50 of 2.5 μM. 2.5 μM Pentamidine induces early programmed cell death in 49.6% of L. infantum promastigotes. 2.5 μM Pentamidine induces a notorious decrease in promastigotes in both G1 and S phases relative to the control-untreated samples (G1:77.0 vs 15.0%; S:11.0 vs 2.4% for control- and pentamidine-treated promastigotes, resp). Pentamidine is able to bind with calf-thymus DNA (CT-DNA) and induces conformational changes in the DNA double helix. Pentamidine also binds with ubiquitin to modifiy the β-cluster of ubiquitin. Pentamidine is an inhibitor of phosphatase of regenerating liver (PRLs). 1 μg/mL of Pentamidine complete inhibits the activity of recombinant PTP1B in dephosphorylating a phos-photyrosine peptide. 10 μg/mL of Pentamidine completely inhibits the activities of recombinant PRL-1, PRL-2 and PRL-3 in dephosphorylating a phosphotyrosine peptide substrate. Incubation with Pentamidine (1 μg/mL) for 48 h reduces the activity of intracellular PRL phosphatases in transfected NIH3T3 cells by more than 85%. 10 μg/mL Pentamidine completely inhibits the growth of melanoma cell line (WM9), prostate carcinoma cell line (DU145 and C4–2), ovarian carcinoma cell line (Hey), colon carcinoma cell line (WM480), and lung carcinoma cell line (A549) which all express endogenous PRLs.

In vivo

Pentamidine has a potent antiprotozoal activity in animal models. Pentamidine (0.3-9 mg/L) decreased the viability of P. carinii in experimental models in chick embryo lung epithelial cells and lung cells of rats with pneumonia. 5 mg/kg Pentamidine treatment for 2 weeks eradicates Pneumocystis carinii pneumonia in 75% of the animals. Pentamidine inhibits the growth of WM9 human melanoma tumors in nude mice. During the 16-week study period, the tumors in 250 μg pentamidine-treated mice stays at sizes similar to those at the treatment initiation point, whereas the tumors in the control mice grow so rapidly that humane sacrifice of the animals is required at the 4th week. Pentamidine induces significant necrosis that accounts for more than 50% of the tumor mass.
Cell Data

cell lines:

Concentrations:0.1-10 μg/mL

Incubation Time:6 days

Powder Purity:≥99%

规格

英文别名
Ethanesulfonic acid, 2-hydroxy-, compd. with 4,4'-[1,5-pentanediylbis(oxy)]bis[benzenecarboximidamide] (2:1)
规格或纯度
10mM in DMSO
英文名称
Pentamidine isethionate
生化机理
喷他脒是 PRL 磷酸酶的抑制剂,还能抑制 DNA、RNA 和蛋白质的合成。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
Kinetoplast DNA 抑制剂
名称和识别符
EC号
205-424-1
分子类型
小分子
Isomeric SMILES
C1=CC(=CC=C1C(=N)N)OCCCCCOC2=CC=C(C=C2)C(=N)N.C(CS(=O)(=O)O)O.C(CS(=O)(=O)O)O
PubChem CID
分子量
592.68

技术文档

📋 安全数据表 (SDS)

全面的危险、操作、储存及法规合规文件。

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批次质量数据。输入批号以获取对应 COA。

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产品规格和应用的快速参考摘要。

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🔬 规格说明书

该级别的完整质量属性和验收标准。

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高级数据

化学和物理性质
溶解性
Solubility (25°C) In vitro Ethanol: mg/mL    
安全和危险性(GHS)
信号词
警告
危险声明

H227: 可燃液体

预防措施声明

P210: 远离热源,热表面,火花,明火和其他点火源。 - 禁止抽烟。

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