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关于此项目
经验公式(希尔记法):
C34H33N3O5
化学文摘社编号:
分子量:
563.64
UNSPSC Code:
12161501
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
依克立达, ≥98% (HPLC)
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL (clear solution, warmed)
shipped in
wet ice
storage temp.
−20°C
SMILES string
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
Application
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
Biochem/physiol Actions
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。
Features and Benefits
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。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
商品
Discover Bioactive Small Molecules for ADME/Tox
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
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
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| SML0486-10MG | 04061837084652 |
| SML0486-50MG | 04061837084669 |