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依克立达盐酸盐

依克立达盐酸盐用途

Elacridar(GF120918; GW0918)盐酸盐是P-糖蛋白抑制剂，在体内外实验中常作为工具化合物。

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依克立达盐酸盐名称

[ CAS 号 ]:
143851-98-3

[ 中文名 ]:
依克立达盐酸盐

[ 英文名 ]:
Elacridar hydrochloride

[英文别名 ]:

UNII-NX2BHH1A5B
Elacridar HCl
Elacridar hydrochloride
Elacridar hydrochloride (USAN)
Elacridar (hydrochloride)

依克立达盐酸盐生物活性

[ 描述 ]:

Elacridar(GF120918; GW0918)盐酸盐是P-糖蛋白抑制剂,在体内外实验中常作为工具化合物。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> P-糖蛋白

研究领域 >> 癌症

[参考文献]

[1]. Sane R, Mittapalli RK, Elmquist WF. Development and evaluation of a novel microemulsion formulation of elacridar to improve its bioavailability. J Pharm Sci. 2013 Jan 18.

[2]. Bankstahl JP, Bankstahl M, Romermann K, et al. Tariquidar and Elacridar Are Dose-Dependently Transported by P-Glycoprotein and Bcrp at the Blood-Brain Barrier: A Small-Animal PET and In-Vitro Study. Drug Metab Dispos. 2013 Jan 10.

[3]. Sane R, Agarwal S, Elmquist WF. Brain distribution and bioavailability of elacridar after different routes of administration in the mouse. Drug Metab Dispos. 2012 Aug;40(8):1612-9.

[4]. Tang SC, Lagas JS, Lankheet NA, et al. Brain accumulation of sunitinib is restricted by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by oral elacridar and sunitinib coadministration. Int J Cancer. 2012 Jan 1;130(1):223-33. doi: 10.1002/ijc.26000.

[5]. Kuppens IE, Witteveen EO, Jewell RC, et al. A phase I, randomized, open-label, parallel-cohort, dose-finding study of elacridar (GF120918) and oral topotecan in cancer patients. Clin Cancer Res. 2007 Jun 1;13(11):3276-85.

[6]. Hong Xiao, et al. Polymeric nanovesicle as simultaneous delivery platform with Doxorubicin conjugation and Elacridar encapsulation for enhanced treatment of multidrug-resistant breast cancer. J. Mater. Chem. B. 2018 Oct.

[相关活性小分子]

依克立达盐酸盐物理化学性质

[ 沸点 ]:
701.6ºC at 760 mmHg

[ 分子式 ]:
C₃₄H₃₄ClN₃O₅

[ 分子量 ]:
600.10400

[ 闪点 ]:
378.1ºC

[ 精确质量 ]:
599.21900

[ PSA ]:
92.89000

[ LogP ]:
6.37310

[ 蒸汽压 ]:
1.57E-19mmHg at 25°C

[ 储存条件 ]:
2-8℃

依克立达盐酸盐安全信息

[ 海关编码 ]:
2934999090

依克立达盐酸盐海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%