Product IntroductionBioactivity英文名:
Deferasirox描述: Deferasirox (CGP-72670) 是一种口服铁螯合剂,用于治疗慢性铁过载。
细胞实验: Deferasirox is dissolved in DMSO. HL-60 or KG-1 cells are treated with 0, 5, 10, 50 μM of deferasirox for 24 or 48 h, and proliferation is determined by an MTT assay[2].
体外活性: Deferasirox口服给药大鼠,至少吸收75%,生物利用度为26%.Deferasirox单药治疗小幅延长IPA小鼠的存活时间.静脉注射和口服Deferasirox在血液循环主要以未改变的形式和其铁络合物存在,Deferasirox有99.2%与血浆蛋白结合.Deferasirox显着改善糖尿病酮症酸中毒或中性粒细胞减少小鼠毛霉菌病的存活率和组织真菌负荷,其效果与脂质体两性霉素B相似.Deferasirox也增强了宿主对毛霉菌病的炎症反应.Deferasirox和脂质体两性霉素B联用时协同提高生存率并降低毛霉菌组织的真菌负荷.
体内活性: Deferasirox体外抗烟曲霉,MIC和MFC分别为25和50 mg/L。Deferasirox有效螯合来自米根霉的铁离子,并在远低于临床可达到的血清水平的浓度下对29种临床分离的Mucorales中的28种体外表现出杀病毒活性。Deferasirox孵育诱导显著抑制NF-κB的活性,并且在40个外周血样品中的28个中以无活性形式胞质内螯合其活性亚基p65。Deferasirox可抑制3种人髓细胞系(K562,U937和HL60),其IC50在17-50 mM。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 50 mg/mL (133.92 mM)
Ethanol : 2 mg/mL (5.35 mM)
关键字:
Bacterial |
chelator |
transfusional |
Inhibitor |
CGP72670 |
inhibit |
available |
ICL-670 |
CGP 72670 |
Ferroptosis |
Deferasirox |
overload |
iron |
orally |
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Alogliptin |
Piperazine Erastin |
Acetylcysteine |
TBHQ |
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RSL3 |
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U-73122相关库:
Drug Repurposing Compound Library |
Approved Drug Library |
FDA-Approved & Pharmacopeia Drug Library |
Drug-induced Liver Injury (DILI) Compound Library |
Clinical Compound Library |
Ferroptosis Compound Library |
EMA Approved Drug Library |
Orally Active Compound Library |
NO PAINS Compound Library |
Bioactive Compound Library