依克立达
依克立达结构式
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常用名 | 依克立达 | 英文名 | elacridar |
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| CAS号 | 143664-11-3 | 分子量 | 563.643 | |
| 密度 | 1.3±0.1 g/cm3 | 沸点 | 701.6±60.0 °C at 760 mmHg | |
| 分子式 | C34H33N3O5 | 熔点 | 216-218℃ | |
| MSDS | 中文版 美版 | 闪点 | 378.1±32.9 °C |
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Effect of drug efflux transporters on placental transport of antiretroviral agent abacavir.
Reprod. Toxicol. 57 , 176-82, (2015) Abacavir is as a frequent part of combination antiretroviral therapy used in pregnant women. The aim of this study was to investigate, using in vitro, in situ and ex vivo experimental approaches, whether the transplacental pharmacokinetics of abacavir is affe... |
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Interaction Studies of Resolvin E1 Analog (RX-10045) with Efflux Transporters.
J. Ocul. Pharmacol. Ther. 31 , 248-55, (2015) Screening interactions of a resolvin E1 analog (RX-10045) with efflux transporters (P-glycoprotein [P-gp], multidrug resistance-associated protein [MRP2], and breast cancer-resistant protein [BCRP]).Madin-Darby canine kidney cells transfected with P-gp, MRP2,... |
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Breast Cancer Resistance Protein and P-Glycoprotein Influence In Vivo Disposition of 11C-Erlotinib.
J. Nucl. Med. 56 , 1930-6, (2015) (11)C-erlotinib is a PET tracer to distinguish responders from nonresponders to epidermal growth factor receptor-targeted tyrosine kinase inhibitors and may also be of interest to predict distribution of erlotinib to tissues targeted for treatment. The aim of... |
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Activation status of the pregnane X receptor influences vemurafenib availability in humanized mouse models.
Cancer Res. 75 , 4573-81, (2015) Vemurafenib is a revolutionary treatment for melanoma, but the magnitude of therapeutic response is highly variable, and the rapid acquisition of resistance is frequent. Here, we examine how vemurafenib disposition, particularly through cytochrome P450-mediat... |
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HZ08 reverse P-glycoprotein mediated multidrug resistance in vitro and in vivo.
PLoS ONE 10(2) , e0116886, (2015) Multidrug efflux transporter P-glycoprotein (P-gp) is highly expressed on membrane of tumor cells and is implicated in resistance to tumor chemotherapy. HZ08 is synthesized and studied in order to find a novel P-gp inhibitor.MDCK-MDR1 monolayer transport, cal... |
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P-Glycoprotein (ABCB1) limits the brain distribution of YQA-14, a novel dopamine D3 receptor antagonist.
Chem. Pharm. Bull. 63 , 512-8, (2015) YQA-14 is a promising agent for treating addiction to cocaine and opioids. However, previous studies have showed there is marked contrast between the relatively small differences in pharmacological action in vivo and the large differences in their respective ... |
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pH Dependent but not P-gp Dependent Bidirectional Transport Study of S-propranolol: The Importance of Passive Diffusion.
Pharm. Res. 32 , 2516-26, (2015) Recent controversial publications, citing studies purporting to show that P-gp mediates the transport of propranolol, proposed that passive biological membrane transport is negligible. Based on the BDDCS, the extensively metabolized-highly permeable-highly so... |
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Inhibition of ABCB1 Overcomes Cancer Stem Cell-like Properties and Acquired Resistance to MET Inhibitors in Non-Small Cell Lung Cancer.
Mol. Cancer Ther. 14 , 2433-40, (2015) Patients with non-small cell lung cancer (NSCLC) EGFR mutations have shown a dramatic response to EGFR inhibitors (EGFR-TKI). EGFR T790M mutation and MET amplification have been recognized as major mechanisms of acquired resistance to EGFR-TKI. Therefore, MET... |
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Aristolochic acid I is a substrate of BCRP but not P-glycoprotein or MRP2.
J. Ethnopharmacol. 172 , 430-5, (2015) Aristolochic acid nephropathy is a severe kidney disease caused by the administration of aristolochic acid, which is widely existed in plants of the Aristolochiaceae family. Aristolochic acid I (AAI) is the main toxic component in aristolochic acid.The roles ... |
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Characterisation and manipulation of docetaxel resistant prostate cancer cell lines.
Mol. Cancer 10 , 126, (2011) There is no effective treatment strategy for advanced castration-resistant prostate cancer. Although Docetaxel (Taxotere®) represents the most active chemotherapeutic agent it only gives a modest survival advantage with most patients eventually progressing be... |