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
登录 查看组织和合同定价。
选择尺寸
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
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)
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
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
Seng Chuan Tang et al.
The Journal of pharmacology and experimental therapeutics, 341(1), 164-173 (2012-01-13)
N-desethyl sunitinib is a major and pharmacologically active metabolite of the tyrosine kinase inhibitor and anticancer drug sunitinib. Because the combination of N-desethyl sunitinib and sunitinib represents total active drug exposure, we investigated the impact of several multidrug efflux transporters
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)
商品
Discover Bioactive Small Molecules for ADME/Tox
我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.
联系客户支持