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依克立达 /Elacridar {[allProObj[0].p_purity_real_show]}

货号:A351095 同义名: GG918;GF120918

Elacridar是一种口服活性 P-糖蛋白 (Pgp) 和乳腺癌耐药蛋白 (BCRP) 抑制剂,用于研究外排转运蛋白对药物在脑中分布的影响,并用于癌症研究。

Elacridar 化学结构 CAS号:143664-11-3
Elacridar 化学结构
CAS号:143664-11-3
Elacridar 3D分子结构
CAS号:143664-11-3
Elacridar 化学结构 CAS号:143664-11-3
Elacridar 3D分子结构 CAS号:143664-11-3
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Elacridar 纯度/质量文件 产品仅供科研

货号:A351095 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 P-gp 其他靶点 纯度
Elacridar BCRP 99%+
Zosuquidar 3HCl ++

P-gp, Ki: 60 nM

99%+
SC144 99%+
Tariquidar +++

P-gp, Kd: 5.1 nM

98%
Schizandrin B 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Elacridar 生物活性

靶点
  • P-gp

描述 The multidrug resistance is an obstacle in the chemotherapy treatment for many solid and haematological tumours. Many factors can cause the multidrug resistance. Among them, the overexpression of P-gp (ABCB1), an ATP-binding cassette (ABC) drug efflux transporter, on the surface of resistant cells is considered as a key factor mediating multidrug resistance. Elacridar is a dual inhibitor of P-gp/BCRP, which can completely inhibit directed transport of crizotinib by P-gp at concentration of 5μM in MDCKII cells expressing human ABCB1. Elacridar is usually used combined with other anticancer drugs to increase the bio-available, achieve higher plasma concentration and improve brain accumulation of these anticancer drugs, such as tyrosine kinase inhibitor (TKI) . Coadministration of elacridar at dose of 100mg/kg could increase the plasma and brain concentrations and brain/plasma ratio of crizotinib in mice, suggesting that the effect of elacridar on increasement of crizotinib oral availability and delivery to the brain[1].

Elacridar 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
Caco-2 cells Function assay Inhibition of human P-gp mediated [3H]vinblastine transport activity in human Caco-2 cells, EC50=2 μM 18276145
HEK293 cells Function assay Inhibition of ABCG2 expressed in HEK293 cells assessed as mitoxantrone-mediated efflux by flow cytometry, IC50=0.41 μM 17317193
Kb-V1 cells Function assay 10 mins Inhibition of ABCB1 expressed in Kb-V1 cells after 10 mins by calcein-AM assay, IC50=0.193 μM 21570282
MCF7/Topo cells Function assay Inhibition of ABCG2 overexpressed in human MCF7/Topo cells by flow cytometric-based mitoxantrone efflux assay, IC50=0.25 μM 19170519

Elacridar 动物研究

Dose Rat: 0.3 mg/kg - 7.5 mg/kg[2] (i.v.); Mice: 100mg/kg[3] (i.p., p.o.)
Administration i.v., i.p., p.o.
Pharmacokinetics
Animal Mice[3]
Dose 2.5 mg/kg (i.v.)
100 mg/kg (i.p.)
100 mg/kg (p.o.)
AUC0→inf 161.4 μg·min/ml (i.v.)
90.3 μg·min/ml(i.p.)
1460 μg·min/ml (p.o.)
AUC0→last 138.6 ± 6.5 μg·min/ml (i.v.)
63.5 ± 6.6 μg·min/ml(i.p.)
792.8 ± 67.9 μg·min/ml (p.o.)
T1/2 4.4 h (i.v.)
4.3 h (i.p.)
20 h (p.o.)
Tmax 0.5 h (i.v.)
0.5 h (i.p.)
8 h (p.o.)
Cmax 0.564 ± 0.14 μg/ml (i.v.)
0.295 ± 0.06 μg/ml (i.p.)
0.78 ± 0.12 μg/ml (p.o.)

Elacridar 参考文献

[1]Kuntner C, Bankstahl JP, et al. Dose-response assessment of tariquidar and elacridar and regional quantification of P-glycoprotein inhibition at the rat blood-brain barrier using (R)-[(11)C]verapamil PET. Eur J Nucl Med Mol Imaging. 2010 May;37(5):942-53.

[2]Sane R, Agarwal S, 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.

Elacridar 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.77mL

0.35mL

0.18mL

8.87mL

1.77mL

0.89mL

17.74mL

3.55mL

1.77mL

Elacridar 技术信息

CAS号143664-11-3
分子式C34H33N3O5
分子量 563.643
别名 GG918;GF120918;GW120918;GW0918
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 4 mg/mL(7.1 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 1 mg/mL clear

PO 0.5% CMC-Na 70 mg/mL suspension

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