推荐产品
产品名称
依克立达, ≥98% (HPLC)
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL (clear solution, warmed)
运输
wet ice
储存温度
−20°C
SMILES字符串
COc1cccc2C(=O)c3cccc(C(=O)Nc4ccc(CCN5CCc6cc(OC)c(OC)cc6C5)cc4)c3Nc12
InChI
1S/C34H33N3O5/c1-40-28-9-5-7-26-32(28)36-31-25(33(26)38)6-4-8-27(31)34(39)35-24-12-10-21(11-13-24)14-16-37-17-15-22-18-29(41-2)30(42-3)19-23(22)20-37/h4-13,18-19H,14-17,20H2,1-3H3,(H,35,39)(H,36,38)
InChI key
OSFCMRGOZNQUSW-UHFFFAOYSA-N
应用
依克立达（Elacridar）可用作：
- 作为化学物质，解释自噬作用与舒尼替尼耐药机制之间的联系
- 作为 ATP 结合盒 B亚家族1成员的抑制剂，研究其对 NSC23766细胞毒性的作用
- 处理罗丹明123（Rh123）标记细胞，在荧光激活细胞分选法（FACS）中设置分选门
生化/生理作用
GF120918（依克立达）是 ABC 转运蛋白 MDR-1 (P-gp) 和 BCRP 的强效抑制剂。GF120918 可增加细胞毒性抗肿瘤药物的生物利用度，也可导致大脑和 CNS 中抗 HIV 药物水平升高。
GF120918（依克立达）是一种 MDR-1 (P-gp) 抑制剂。
特点和优势
这种化合物是 ADME 毒性研究的特色产品。点击此处发现更多特色 ADME 毒性产品。在sigma.com/discover-bsm可了解更多关于生物活性小分子的其他研究领域。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Akash Chaurasiya et al.
Journal of microencapsulation, 29(6), 583-595 (2012-03-24)
In the present work, concomitant use of self-microemulsifying drug delivery systems (SMEDDS) and a novel third-generation P-gp inhibitor, GF120918 (elacridar), for the effective transport of taxanes (paclitaxel and docetaxel) across an in vitro model of the intestinal epithelium and uptake into
C Gadeyne et al.
Journal of veterinary pharmacology and therapeutics, 34(5), 417-423 (2011-01-19)
The influence of pretreatment with ketoconazole [cytochrome P450 3A (CYP3A) + P-glycoprotein (P-gp) inhibitor], elacridar (selective P-gp inhibitor) and rifampicin (CYP3A + P-gp inducer) on oral morphine pharmacokinetics and pharmacodynamics was investigated in experimental dogs. Seven beagles were used in
Selvi Durmus et al.
Molecular pharmaceutics, 9(11), 3236-3245 (2012-10-02)
Vemurafenib (PLX4032) is a novel tyrosine kinase inhibitor that has clinical efficacy against metastatic melanoma harboring a BRAF(V600E) mutation. We aimed to establish whether oral availability and brain penetration of vemurafenib could be restricted by the multidrug efflux transporters P-glycoprotein
Ramola Sane et al.
The Journal of pharmacology and experimental therapeutics, 345(1), 111-124 (2013-02-12)
The study objective was to investigate factors that affect the central nervous system (CNS) distribution of elacridar. Elacridar inhibits transport mediated by P-glycoprotein (P-gp) and breast cancer resistance protein (Bcrp) and has been used to study the influence of transporters
Stéphanie Chasseigneaux et al.
Fluids and barriers of the CNS, 21(1), 33-33 (2024-04-09)
The blood-brain barrier (BBB) is pivotal for the maintenance of brain homeostasis and it strictly regulates the cerebral transport of a wide range of endogenous compounds and drugs. While fasting is increasingly recognized as a potential therapeutic intervention in neurology
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