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:
产品名称
依克立达, ≥98% (HPLC)
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
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
Quality Level
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
Tomoteru Yamasaki et al.
Nuclear medicine and biology, 38(5), 707-714 (2011-07-02)
Topotecan (TPT) is a camptothecin derivative and is an anticancer drug working as a topoisomerase-I-specific inhibitor. But TPT cannot penetrate through the blood-brain barrier. In this study, we synthesized a new positron emission tomography (PET) probe, [(11)C]TPT, to evaluate the
Christopher Rowbottom et al.
Pharmacology research & perspectives, 9(2), e00740-e00740 (2021-03-05)
Transporters can play a key role in the absorption, distribution, metabolism, and excretion of drugs. Understanding these contributions early in drug discovery allows for more accurate projection of the clinical pharmacokinetics. One method to assess the impact of transporters in
Thomas Wanek et al.
European journal of nuclear medicine and molecular imaging, 39(1), 149-159 (2011-10-11)
One important mechanism for chemoresistance of tumours is overexpression of the adenosine triphosphate-binding cassette transporter P-glycoprotein (Pgp). Pgp reduces intracellular concentrations of chemotherapeutic drugs. The aim of this study was to compare the suitability of the radiolabelled Pgp inhibitors [(11)C]tariquidar
Hanneke G M Wittgen et al.
Molecular pharmaceutics, 9(5), 1351-1360 (2012-03-21)
Although the CB1 receptor antagonist/inverse agonist rimonabant has positive effects on weight loss and cardiometabolic risk factors, neuropsychiatric side effects have prompted researchers to develop peripherally acting derivatives. Here, we investigated for a series of 3,4-diarylpyrazoline CB1 receptor antagonists if
The xenobiotic transporter Mdr1 enforces T cell homeostasis in the presence of intestinal bile acids
Cao W, et al.
Immunity, 47(6), 1182-1196 (2017)
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