Elacridar
目录号: PL05093 纯度: ≥99%
CAS No. :143664-11-3
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中文名称
Elacridar
中文别名
依克立达;N-[4-[2-(6,7-二甲氧基-3,4-二氢-1H-异喹啉-2-基)乙基]苯基]-5-甲氧基-9-氧代-10H-吖啶-4-甲酰胺;1,2-二氢-5-苯基吡唑-3-酮;1H-吡唑-3,5-二胺盐酸盐;Elacridar (GF120918) 抑制剂;N-[4-[2-(3,4-二氢-6,7-二甲氧基-2(1H)-异喹啉基)乙基]苯基]-9,10-二氢-5-甲氧基-9-氧代-4-吖啶甲酰胺
英文名称
Elacridar
英文别名
Elacridar;N-[4-[2-(6,7-Dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]-5-methoxy-9-oxo-10H-acridine-4-carboxamide;N-(4-(2-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)-phenyl)-5-methoxy-9-oxo-9,10-dihydroacridine-4-carboxamide;N-[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-4-Acridinecarboxamide;GF120918;GF-120918;GG918;GW0918;GW120918;Elacridar (GF120918);GG 918;GF 120918;AK133066;N488540F94;Elacridar [INN];N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-4-acridinecarboxamide
Cas No.
143664-11-3
分子式
C34H33N3O5
分子量
563.64
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Elacridar 是一种具有口服活性的的 P-glycoprotein (Pgp) 和 乳腺癌抗性蛋白 (BCRP) 抑制剂。Elacridar 可用于检测外排转运体对药物脑内分布的影响以及癌症的研究。
生物活性
Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on drug distribution to brain and the research of cancer.
性状
Solid
IC50 & Target[1][2]
P-glycoprotein (Pgp), BCRP
体外研究(In Vitro)
Elacridar (0.001-1 μM; 2 h) inhibits cell viability of 786-O cells.
Elacridar (5 μM; 24 h) affects P-glycoprotein and ABCG2 protein expression levels in MCF-7 and 786-O cell lines.
Elacridar (5 μM; 24 h) affects Tc-MIBI intracellular accumulation in MCF-7 and 786-O cells. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)
Elacridar (100 mg/kg; i.p. once) shows different distribution in brain and plasma.
1.19 Plasma Pharmacokinetic Parameters of Elacridar in mice.
Mice
PO 100 mg/kg Mice
IP 100
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Sane R, et al. Brain distribution and bioavailability of elacridar after different routes of administration in the mouse. Drug Metab Dispos. 2012 Aug;40(8):1612-9.
[2]. Sato H, et al. Elacridar enhances the cytotoxic effects of sunitinib and prevents multidrug resistance in renal carcinoma cells. Eur J Pharmacol. 2015 Jan 5;746:258-66.
溶解度数据
In Vitro: DMSO : 5 mg/mL (8.87 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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