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。
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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。 |
靶点 |
|
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]. |
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 | ||
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 |
|
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 |
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 |