Deferasirox (ICL-670), 铁螯合剂

CAS: 201530-41-8 货号: D407865 分子式: C21H15N3O4 分子量: 373.36 EC号: 685-491-5
有货
级别和纯度: 10mM in DMSO
别名
地拉罗司(ICL-670)
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
D407865-1ml
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¥613.90
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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

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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 5 篇同行评审文献引用。

概述

Deferasirox(Exjade) is a rationally-designed oral iron chelator. Its main use is to reduce chronic iron overload in patients who are receiving long-term blood transfusions for conditions such as beta-thalassemia and other chronic anemias. The half-life of deferasirox is between 8 and 16 hours allowing once a day dosingA tridentate chelator that binds iron with high affinity

Information

Deferasirox (ICL-670) Deferasirox (ICL-670, CGP-72670) is an iron chelator , also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor , and Cytochrome P450 1A2 inhibitor. Deferasirox-induced iron depletion promotes BclxL downregulation and cell
In vitro

Deferasirox effectively chelates iron from Rhizopus oryzae and demonstrates cidal activity in vitro against 28 of 29 clinical isolates of Mucorales at concentrations well below clinically achievable serum levels. Deferasirox incubation induces a significant inhibition of NF-κB activity and a cytoplasmic sequestration of its active subunit p65 in an inactive form in 28 of 40 peripheral blood samples. Deferasirox inhibits three human myeloid cell lines (K562, U937, and HL60) with IC50 of 17-50 mM. Deferasirox is cidal in vitro against A. fumigatus, with an MIC and MFC of 25 and 50 mg/L, respectively.

In vivo

Deferasirox significantly improves survival and decreased tissue fungal burden in diabetic ketoacidotic or neutropenic mice with mucormycosis, with an efficacy similar to that of liposomal amphotericin B. Deferasirox treatment also enhances the host inflammatory response to mucormycosis. Deferasirox synergistically improves survival and reduces tissue fungal burden when combined with liposomal amphotericin B. Deferasirox administered p.o. to rats is absorbed to at least 75%, and the bioavailability is 26%.Deferasirox is present in the blood circulation mainly in the unchanged form and as its iron complex, Fe(deferasirox)2, after intravenous and p.o. administration. Deferasirox is 99.2% bound to plasma proteins. Deferasirox monotherapy modestly prolongs survival of mice with IPA.
Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥99%

规格

别名
地拉罗司(ICL-670)
英文别名
CGP-72670 | 4-​[3,​5-​bis(2-​hydroxyphenyl)​-​1H-​1,​2,​4-​triazol-​1-​yl]​-benzoic acid
规格或纯度
10mM in DMSO
英文名称
Deferasirox (ICL-670)
生化机理
地拉罗司(ICL-670,CGP-72670)是一种铁螯合剂,也是细胞色素 P450 3A4 诱导剂、细胞色素 P450 2C8 抑制剂和细胞色素 P450 1A2 抑制剂。地拉罗司诱导的铁耗竭会促进 BclxL 下调和细胞死亡。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
螯合剂
作用机制
铁螯合剂
名称和识别符
EC号
685-491-5
分子类型
小分子
Isomeric SMILES
C1=CC=C(C(=C1)C2=NN(C(=N2)C3=CC=CC=C3O)C4=CC=C(C=C4)C(=O)O)O
分子量
373.36
Reaxy-Rn
8442898
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8442898&ln=

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高级数据

产品属性
ALogP 3.8
化学和物理性质
熔点
262 °C
安全和危险性(GHS)
信号词
警告
危险声明

H302: 吞食有害

H373: 通过长时间或反复暴露对器官造成损害

H410: 对水生生物有剧毒并具有长期持续影响

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