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CAS No.: 143664-11-3
Synonyms: GF120918;GW0918;GG918
Elacridar is a P-glycoprotein inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules.
生物活性
动物研究 | |||||||||||||||
剂量 | Rat: 0.3 mg/kg - 7.5 mg/kg[2] (i.v.); Mice: 100mg/kg[3] (i.p., p.o.) | ||||||||||||||
给药途径 | i.v., i.p., p.o. | ||||||||||||||
动物药代数据 |
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实验方案
技术信息
CAS号 | 143664-11-3 | 储存条件 |
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分子式 | C34H33N3O5 | 运输 | 蓝冰 | |||||||||||||
分子量 | 563.64 | 别名 | GF120918;GW0918;GG918;GW120918;依克立达 | |||||||||||||
溶解度 |
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动物实验配方 |
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Cell Lines | Concentration | Assay Type | Time | Activity Description | Data Sources |
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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 |
MDCK cells | - | Function assay | - | Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay, IC50=0.43 μM | 19932960 |
MDCK2-MDR1 cells | - | Function assay | 60 mins | Inhibition of human Pgp overexpressed in human MDCK2-MDR1 cells assessed as inhibition of R123 efflux after 60 mins, IC50=0.4 μM | 21419632 |
SKOV3 cells | - | Cytotoxicity assay | - | Cytotoxicity against human SKOV3 cells, IC50=8.1 μM | 11754602 |
SKVLB1 cells | - | Cytotoxicity assay | - | Cytotoxicity against human multidrug-resistant SKVLB1 cells in presence of adriamycin, IC50=0.02 μM | 11754602 |
SKVLB1 cells | - | Cytotoxicity assay | - | Cytotoxicity against human multidrug-resistant SKVLB1 cells, IC50=1.4 μM | 11754602 |
靶点 | Description | IC50 |
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