Výsledky vyhledávání - "Christine C. Orozco"

Evaluation of Prediction Accuracy for Volume of Distribution in Rat and Human Using In Vitro, In Vivo, PBPK and QSAR Methods

Autor: Shibin Mathew, George Chang, Christopher Keefer, Shinji Yamazaki, Jian Lin, Samantha Jordan, Woodrow Burchett, Christine C. Orozco, David A. Tess, Nathaniel Woody, Rhys M. Jones, Li Di

Publikováno v: Journal of pharmaceutical sciences. 110(4)

Volume of distribution at steady state (Vss) is an important pharmacokinetic parameter of a drug candidate. In this study, Vss prediction accuracy was evaluated by using: (1) seven methods for rat with 56 compounds, (2) four methods for human with 12

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cc076581837f9da92c421f3c57955317
https://pubmed.ncbi.nlm.nih.gov/33338491

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In Vitro Characterization of Ertugliflozin Metabolism by UDP-Glucuronosyltransferase and Cytochrome P450 Enzymes

Autor: Jian Lin, Kimberly Lapham, Ernesto Callegari, Julie Cianfrogna, Christine C. Orozco, Raman Sharma, Mark Niosi, Theunis C. Goosen

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 48(12)

Ertugliflozin is primarily cleared through UDP-glucurosyltransferase (UGT)–mediated metabolism (86%) with minor oxidative clearance (12%). In vitro phenotyping involved enzyme kinetic characterization of UGTs or cytochrome P450 enzymes catalyzing f

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c5f829ffbea55140205a3e462fa347f3
https://pubmed.ncbi.nlm.nih.gov/33020067

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6-Chloro-5-[4-(1-Hydroxycyclobutyl)Phenyl]-1H-Indole-3-Carboxylic Acid is a Highly Selective Substrate for Glucuronidation by UGT1A1, Relative toβ-Estradiol

Autor: Kimberly Lapham, Jian Lin, Jonathan J. Novak, Heather Eng, Theunis C. Goosen, Li Di, Amit S. Kalgutkar, Kimberly O. Cameron, Mark Niosi, Christine C. Orozco, Sangwoo Ryu, Keith Riccardi

Publikováno v: Drug Metabolism and Disposition. 46:1836-1846

6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic acid (PF-06409577) is a direct activator of the human β1-containing adenosine monophosphate-activated protein kinase (ΑMPK) isoforms. The clearance mechanism of PF-06409577 in animal

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8a21e8671f0b104eab298f3d27ba8a2f
https://doi.org/10.1124/dmd.118.083709

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Structural attributes influencing unbound tissue distribution

Autor: Li Di, David A. Tess, Jian Lin, Kevin J. Filipski, Sangwoo Ryu, Karen Atkinson, Keith Riccardi, Dennis O. Scott, Christopher Keefer, Amit S. Kalgutkar, George Chang, Robert K. Mongillo, John Litchfield, Christine C. Orozco

Publikováno v: European Journal of Medicinal Chemistry. 185:111813

Unbound tissue-to-plasma partition coefficients (Kpuu) were determined for 56 structurally diverse compounds in rats following intravenous infusion. Five tissues were included in the study: white adipose, brain, heart, liver, and skeletal muscle. The

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c0b181dd9d8b401c0c1f40dcb2c82c82
https://doi.org/10.1016/j.ejmech.2019.111813

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Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization

Autor: Jotham Wadsworth Coe, Brajesh K. Rai, Sidney Liang, Keith Dlugolenski, Jennifer E. Davoren, Erik Alphie Lachapelle, Rebecca E. O’Connor, Deane M. Nason, Christine C. Orozco, David Gray, Rouba Kozak, Christopher John Helal, Brian Samas, Yue Liu, Michelle A. Salafia, Anthony R. Harris, Wenjian Xu

Publikováno v: Journal of medicinal chemistry. 61(24)

The discovery of D1 subtype-selective agonists with drug-like properties has been an enduring challenge for the greater part of 40 years. All known D1-selective agonists are catecholamines that bring about receptor desensitization and undergo rapid m

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b084e9e7a5c6d066edd7c22acfa061cd
https://pubmed.ncbi.nlm.nih.gov/30431269

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Discovery of Potent and Selective Periphery-Restricted Quinazoline Inhibitors of the Cyclic Nucleotide Phosphodiesterase PDE1

Autor: Eddie Yang, Jennifer L. Liras, Christine C. Orozco, Christopher W. am Ende, Matthew A. Movsesian, Jayvardhan Pandit, John M. Humphrey, Stephen Jenkinson, Frank S. Menniti, Thomas Allen Chappie, Spiros Liras, Stacey L. Becker, Felix Vajdos, Fabrice Vandeput

Publikováno v: Journal of medicinal chemistry. 61(10)

We disclose the discovery and X-ray cocrystal data of potent, selective quinazoline inhibitors of PDE1. Inhibitor (S)-3 readily attains free plasma concentrations above PDE1 IC50 values and has restricted brain access. The racemic compound 3 inhibits

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aad70863e6c50adf198b09386b95c77c
https://pubmed.ncbi.nlm.nih.gov/29718668

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In Vitro–In Vivo Correlation for Low-Clearance Compounds Using Hepatocyte Relay Method

Autor: Li Di, R. Scott Obach, Carrie Funk, Jian Lin, Christine C. Orozco, Hui Zhang, Beijing Tan, Thomas S. McDonald, Cheng Chang, Karen Atkinson

Publikováno v: Drug Metabolism and Disposition. 41:2018-2023

In vitro-in vivo correlation (IVIVC) of intrinsic clearance in preclinical species of rat and dog was established using the hepatocyte relay method to support high-confidence prediction of human pharmacokinetics for low-clearance compounds. Good IVIV

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2372c92d91c07410717fce1045d02e5
https://doi.org/10.1124/dmd.113.053322

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