SML0486
依克立达
≥98% (HPLC), powder, ABC transporters MDR-1 (P-gp) inhibitor
别名:
GF120918, GG918, GW0918, N-[4-[2-（3,4-二氢-6,7-二甲氧基-2 (1H)-异喹啉基）乙基] 苯基]-9,10-二氢-5-甲氧基-9-氧代-4-吖啶甲酰胺
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About This Item
经验公式（希尔记法）:
C34H33N3O5
CAS号:
分子量:
563.64
MDL编号:
UNSPSC代码:
12161501
PubChem化学物质编号:
NACRES:
NA.77
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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)
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
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
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
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
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
Nico Holmstock et al.
Molecular pharmaceutics, 10(3), 1056-1062 (2013-01-31)
Rodent models are less suitable for predicting drug-drug interactions at the level of the human intestinal mucosa, especially when nuclear receptors such as pregnane X receptor (PXR) are involved. Recently, a transgenic mouse model, expressing both human PXR and CYP3A4
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