3h e217βg

Manufactured by PerkinElmer

[3H]-E217βG is a tritium-labeled estradiol-17β-glucuronide compound. It is a radiotracer used in research applications to study estradiol metabolism and pharmacokinetics.

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Lab products found in correlation

3h e1s, by PerkinElmer (2 mentions) Unlabeled e217βg, by Merck Group (2 mentions) Bio safe 2 liquid scintillation mixture, by Research Products International (2 mentions) 3h taurocholic acid, by PerkinElmer (1 mentions) Cck 8, by Merck Group (1 mentions) 3h docetaxel, by American Radiolabeled Chemicals (1 mentions) Docetaxel, by LC Laboratories (1 mentions) Insulin transferrin selenium, by BD (1 mentions) Dulbecco s modified eagle medium dmem, by Merck Group (1 mentions) Fetal bovine serum (fbs), by Cytiva (1 mentions) Triton x 100, by Merck Group (1 mentions) Rifampicin, by Merck Group (1 mentions) Antibiotic antimycotic solution, by Merck Group (1 mentions) Dasatinib, by LC Laboratories (1 mentions) Matrigel, by BD (1 mentions) William s e medium, by Thermo Fisher Scientific (1 mentions) Cm3000, by Thermo Fisher Scientific (1 mentions) 3h taurocholate, by PerkinElmer (1 mentions) Matrigel, by Corning (1 mentions) 3h digoxin, by PerkinElmer (1 mentions)

Close spelling variants of this product

[3H]-estradiol 17 β-D-glucuronide (E217βG)

5 protocols using 3h e217βg

Radiolabeled Compounds for Receptor Binding

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[³H]-docetaxel (60 Ci/mmol) and [³H]-xanthine (19.4 Ci/mmol) were purchased from American Radiolabeled Chemicals (St Louis, MO). [³H]-E₂17βG (45 Ci/mmol), [³H]-E₁S (46 Ci/mmol), [³H]-taurocholic acid (5.0 Ci/mmol), and [¹⁴C]-tetraethylammonium (3.2 mCi/mmol) were purchased from PerkinElmer Life and Analytical Sciences (Boston, MA). [³H]-CCK-8 (77 Ci/mmol) was purchased from Amersham Pharmacia Biotech (Buckinghamshire, UK). Unlabeled E₂17βG, E₁S, and CCK-8 were purchased from Sigma-Aldrich (St Louis, MO), and docetaxel was purchased from LC Laboratories (Woburn, MA). All other chemicals were of analytical grade and are commercially available.

Yamada A., Maeda K., Kiyotani K., Mushiroda T., Nakamura Y, & Sugiyama Y. (2014). Kinetic Interpretation of the Importance of OATP1B3 and MRP2 in Docetaxel-Induced Hematopoietic Toxicity. CPT: Pharmacometrics & Systems Pharmacology, 3(7), e126-.

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Radioligand Binding Assay Protocol

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[3H]-E₂17βG (specific activity 41.4 Ci/mmol) and [³H]-E₁S (specific activity 54.0 Ci/mmol) were purchased from Perkin Elmer Life Science (Waltham, MA). Dasatinib and CsA were purchased from LC laboratories (Woburn, MA, USA). Rifampicin, unlabeled E₂17βG, Hanks’ balanced salt solution (HBSS), dimethyl sulfoxide (DMSO), Triton X-100, Dulbecco’s Modified Eagle Medium (DMEM), Dulbecco’s phosphate buffered saline (DPBS), trypsin-EDTA solution, and antibiotic antimycotic solution were purchased from Sigma-Aldrich (St. Louis, MO). Poly-L-lysine was purchased from Trevigen Inc. (Gaithersburg, MD). Geneticin^® (G418), BioCoat^™ culture plates, insulin/transferrin/selenium (ITS⁺), and Matrigel^™ were purchased from BD Biosciences (Bedford, MA). Fetal bovine serum (FBS) was purchased from Hyclone Laboratories (Logan, Utah). Bio-Safe II liquid scintillation mixture was purchased from Research Products International (Mt. Prospect, IL).

Pahwa S., Alam K., Crowe A., Farasyn T., Neuhoff S., Hatley O., Ding K, & Yue W. (2017). Pretreatment with Rifampicin and Tyrosine Kinase Inhibitor Dasatinib Potentiates the Inhibitory Effects toward OATP1B1- and OATP1B3-Mediated Transport without Affecting Plasma Membrane Localization of the Transporters. Journal of pharmaceutical sciences, 106(8), 2123-2135.

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Establishing Hepatocyte Culture Models

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Cryopreserved hepatocyte recovery medium (CHRM), primary hepatocyte maintenance supplement (CM3000), and William’s E medium (WEM) were purchased from Thermo Fisher Scientific (Waltham, MA, USA). Human 3 donor pooled liver total RNA (Lot ID. 1402003) was obtained from Clontech (Mountain View, CA, USA). Insulin-transferrin-selenium (ITS) liquid medium was obtained from Sigma-Aldrich (St. Louis, MI, USA). Matrigel and Transwell™ permeable supports made of polyethylene terephthalate (pore size 0.4 μm) were obtained from Corning (Cambridge, MA, USA). [³H]E₂17βG (50 Ci/mmol), [³H]taurocholate (15.4 Ci/mmol), [³H]digoxin (23.8 Ci/mmol), and [¹⁴C]metformin (58 mCi/mmol) were purchased from PerkinElmer (Waltham, MA). All other chemicals used were commercially available and of reagent grade.

Arakawa H., Nakazono Y., Matsuoka N., Hayashi M., Shirasaka Y., Hirao A, & Tamai I. (2023). Induction of open-form bile canaliculus formation by hepatocytes for evaluation of biliary drug excretion. Communications Biology, 6, 866.

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Radioactive Labeling and Inhibitor Protocol

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[³H]E₂17βG (specific activity 41.4 Ci/mmol) and ³²P-orthophosphate (10 mCi) were purchased from PerkinElmer Life Science (Waltham, MA). Complete protease inhibitor cocktail tablets, Phosstop phosphatase inhibitor tablets were purchased from Roche Diagnostics (Indianapolis, IN). Geneticin (G418) and EZ-Link™ Sulfo-NHS-SS-Biotin were purchased from Thermo Fisher Scientific (Carlsbad, CA). Protein A/G beads were purchased from Santa Cruz Biotechnology (Dallas, TX). Unlabeled estradiol 17β-glucuronide (E₂17βG), lactic acid dehydrogenase (LDH) cytotoxicity kit and fetal bovine serum (FBS) were purchased from Sigma Aldrich (St. Louis, MO). Bio-Safe II liquid scintillation mixture and 1,4-dithiothreitol (DTT) were purchased from Research Products International (Mt. Prospect, IL). Other reagents, unless specified, were purchased from Sigma Aldrich (St. Louis, MO), Thermo Fisher Scientific (Carlsbad, CA), or VWR International (Radnor, PA).

Crowe A., Zheng W., Miller J., Pahwa S., Alam K., Fung K.M., Rubin E., Yin F., Ding K, & Yue W. (2019). Characterization of plasma membrane localization and phosphorylation status of organic anion transporting polypeptide (OATP) 1B1 c.521 T>C nonsynonymous single-nucleotide polymorphism. Pharmaceutical research, 36(7), 101.

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MRP4-Mediated E217βG Transport Assay

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HEK293T cells were transiently transfected with a pcDNA3.1 vector containing human MRP4 cDNA as previously described (14) . Production of inside-out membrane vesicles enriched for MRP4, and measurement of ATP-dependent transport of [ 3 H]E217βG (specific activity 34.3 Ci/mmol; Perkin Elmer) conducted as previously described (14) . Transport in the presence of AMP was subtracted from transport in the presence of ATP and reported as ATP-dependent [ 3 H]E217βG uptake. Transport levels in vesicles prepared from untransfected HEK293T cells was 8% of that from MRP4-enriched vesicles.

Huynh T., Murray J., Flemming C.L., Kamili A., Hofmann U., Cheung L., Roundhill E.A., Yu D.M.T., Webber H.T., Schwab M., Henderson M.J., Haber M., Norris M.D, & Fletcher J.I. (2020). CCI52 sensitizes tumors to 6-mercaptopurine and inhibits MYCN-amplified tumor growth. Biochemical pharmacology, 172.

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