The chemical compounds under investigation, zosuquidar, tariquidar and elacridar were purchased from Selleck Chemicals (Houston, TX), MedKoo Biosciences (Chapel Hill, NC), and Sigma-Aldrich Chemical Co. (St. Louis, MO), respectively. Cyclosporine A was obtained from Alexis Corporation (Lausen, Switzerland). The radioactive compound [125I]iodoarylazidoprazosin (IAAP) (2200 Ci/mmol) was purchased from PerkinElmer Life Sciences (Boston, MA). The fluorescent compounds calcein-AM, bodipy-FLprazosin and bodipy-paclitaxel were purchased from Invitrogen (Carlsbad, CA). NBD-cyclosporine A was generously provided by Drs. Anika Hartz and Björn Bauer, University of Minnesota (Duluth, MN). ATP, valinomycin and all other chemicals were obtained from Sigma-Aldrich Chemical Co. (St. Louis, MO). The P-gp specific monoclonal antibody C219 was supplied by Fujirebio Diagnostic Inc. (Malvern, PA); while the antibodies used for flow cytometry studies MRK16 and UIC2 were purchased from Kyowa Medex Company (Tokyo, Japan) and eBioscience (San Diego, CA), respectively. FITC-labeled anti-mouse secondary antibody IgG2a was obtained from BD Biosciences (San Jose, CA).
Elacridar
Manufactured by Selleck Chemicals
Sourced in China, Germany, United States
Elacridar is a laboratory equipment product that functions as a P-glycoprotein inhibitor. It is designed to facilitate the investigation of drug transport and bioavailability in various experimental settings.
Automatically generated - may contain errors
Lab products found in correlation
Mln4924, by Chemietek (2 mentions)
Ko143, by Cayman Chemical (2 mentions)
Thz531, by Cayman Chemical (2 mentions)
Cudc 101, by MedChemExpress (2 mentions)
Pf 3758309, by Apexbio (2 mentions)
Gedatolisib, by Apexbio (2 mentions)
Ks176, by MedChemExpress (2 mentions)
Mln7243, by Chemietek (2 mentions)
Mitoxantrone, by Merck Group (2 mentions)
Tariquidar, by MedChemExpress (2 mentions)
Valinomycin, by Merck Group (1 mentions)
Fitc labeled anti mouse secondary antibody igg2a, by BD (1 mentions)
125i iodoarylazidoprazosin iaap 2200 ci mmol, by PerkinElmer (1 mentions)
Calcein am, by Thermo Fisher Scientific (1 mentions)
Bodipy paclitaxel, by Thermo Fisher Scientific (1 mentions)
Zosuquidar, by Selleck Chemicals (1 mentions)
Tariquidar, by Selleck Chemicals (1 mentions)
Horseradish peroxidase hrp conjugated goat anti rabbit, by Beyotime (1 mentions)
Lenvatinib, by MedChemExpress (1 mentions)
T40044, by Abmart (1 mentions)
7 protocols using elacridar
1
Characterization of P-gp Inhibitors
2
Synthesis of Karonudib and Elacridar
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Karonudib (TH1579) was synthesized at the Karolinska Institute according to previously published synthesis schemes (WO2015187088A1). Elacridar (GF120918) was bought from Selleck Chem (selleckchem.com).
3
Elacridar and Combination Therapy
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Lenvatinib (HY-10981), gefitinib (HY-50895), and copanlisib (HY-15346A) were purchased from MedChemExpress (Shanghai, China), and elacridar (S7772) was purchased from Selleck Chemicals (Shanghai, China). Stock solutions of 20 mM Lenvatinib, 100 mM elacridar, and 20 mM gefitinib were dissolved in 100% dimethyl sulfoxide (DMSO), and the stock solution of 10 mM copanlisib was dissolved in Milli-Q water. Antibodies against total epidermal growth factor receptor (EGFR; A11577, ABclonal), phospho-EGFR (AP0820, ABclonal), total PI3K (ab32089, Abcam), phospho-PI3K (4228, CST), total AKT (9272, CST), phospho-AKT (4060, CST), total MEK1/2 (A4868, ABclonal), phospho-MEK1/2 (AP0209, ABclonal), total ERK1/2 (4695, CST), phospho-ERK1/2 (4376, CST), caspase-3 (T40051, Abmart), Bcl-2-associated X (Bax; T40044, Abmart), multidrug resistance protein 1 (MDR1; 13978, CST), breast cancer resistance protein (BCRP; 130244, Abcam), and glyceraldehyde 3-phosphate dehydrogenase (GAPDH; 5174, CST) were used. Horseradish peroxidase (HRP)-conjugated goat anti-rabbit and goat anti-mouse antibodies were purchased from Beyotime Biotechnology (Shanghai, China). Alexa Fluor-conjugated goat anti-rabbit (647 nm) and goat anti-mouse (488 nm) antibodies were purchased from Invitrogen (Shanghai, China).
4
Drug Screening for Lysosomal Targeting
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Nintedanib, elacridar and chloroquine were purchased from Selleckchem (Munich, Germany). LysoTracker® Red was obtained from Thermo Fisher Scientific (Waltham, MA, USA), bafilomycin A1 was purchased from Sigma.
5
Detailed Compound Sourcing Protocol
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Mitoxantrone was obtained from Sigma-Aldrich (St. Louis, MO). Pheophorbide a was from Frontier Specialty Chemicals (Logan, UT). MLN-7243 and MLN-4924 were purchased from ChemieTek (Indianapolis, IN). THZ531 and Ko143 were obtained from Cayman Chemical (AnnArbor, MI). PF-3758309 and Gedatolisib were from ApexBio Technology (Houston, TX). CUDC-101, KS176 and tariquidar were from MedChem Express (Monmouth Junction, NJ). Elacridar was from Selleck chemicals (Houston, TX).
6
Transwell-Based Urate Transport Analysis
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A modified Transwell model was used to analyze urate transport. The filter of the Transwell chamber was a polycarbonate membrane separation medium with a pore size of < 5 µM. After precooling, Matrigel was coated onto the surface of the upper chamber, and Caco-2 cells were cultured for 21 days. The resistance test verified the completeness of the monolayer cell membrane. Two hundred microliters of Hanks solution containing 0.1% BSA was added to the AP side (apical hole) as the intestinal lumen side to reduce the nonspecific adsorption of Caco-2 cells to urate and interventions, and 400 µL of Hanks solution containing urate (with 10− mol/L EB or EB and 5 mmol/L elacridar (Selleckchem, Houston, TX, USA, dissolved in DMSO)) was added to the BL side (basolateral hole) as the base side, after which a resistance test was also carried out. We then placed the 24-well plate with the Transwell chamber in a 37 °C incubator and set different time points to draw 200 µL of the receiving solution from the inner well for testing or freeze-storage at − 20 °C. The operated wells were filled with the corresponding volume of Hanks solution containing 0.1% BSA at 37 °C with a maintained pH of approximately 7.4. The experiment was repeated three times.
7
Acquisition of Diverse Chemical Compounds
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Mitoxantrone was obtained from Sigma-Aldrich (St. Louis, MO). Pheophorbide a was from Frontier Specialty Chemicals (Logan, UT). MLN-7243 and MLN-4924 were purchased from ChemieTek (Indianapolis, IN). THZ531 and Ko143 were obtained from Cayman Chemical (AnnArbor, MI). PF-3758309 and Gedatolisib were from ApexBio Technology (Houston, TX). CUDC-101, KS176 and tariquidar were from MedChem Express (Monmouth Junction, NJ). Elacridar was from Selleck chemicals (Houston, TX).
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