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Merck
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重要文件

SML0486

Sigma-Aldrich

依克立达

≥98% (HPLC), powder, ABC transporters MDR-1 (P-gp) inhibitor

同義詞:

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

經驗公式(希爾表示法):
C34H33N3O5
CAS號碼:
分子量::
563.64
MDL號碼:
分類程式碼代碼:
12161501
PubChem物質ID:
NACRES:
NA.77

產品名稱

依克立达, ≥98% (HPLC)

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL (clear solution, warmed)

運輸包裝

wet ice

儲存溫度

−20°C

SMILES 字串

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 密鑰

OSFCMRGOZNQUSW-UHFFFAOYSA-N

應用

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。

特點和優勢

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。

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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分析證明 (COA)

Lot/Batch Number

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存取文件庫

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
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
Resistance to sunitinib in renal clear cell carcinoma results from sequestration in lysosomes and inhibition of the autophagic flux
Giuliano S, et al.
Autophagy, 11(10), 1891-1904 (2015)
Ramola Sane et al.
Journal of pharmaceutical sciences, 102(4), 1343-1354 (2013-01-22)
The study objective was to develop a formulation of elacridar to overcome its dissolution-rate-limited bioavailability. Elacridar is a P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor that has been used to improve the brain distribution of drugs that are
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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