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Merck
CN

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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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:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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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



历史批次信息供参考:

分析证书(COA)

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商品

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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
SML0486-10MG04061837084652
SML0486-50MG04061837084669