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Predicting apparent passive permeability of Caco

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Using Microseismicity to Estimate Formation Permeability

Estimates of apparent permeability from both approaches are within the same order of magnitude between 10 mD and 100 mD.Note that we use the term apparent permeability for two reasons.First,the permeability estimates are typically higher than the true formation permeability through enhancement via hydraulic stimulation.Some results are removed in response to a notice of local law requirement.For more information,please see here.Previous123456NextSome results are removed in response to a notice of local law requirement.For more information,please see here.12345NextPredicting apparent passive permeability of Caco-2 and Predicting apparent passive permeability of Caco-2 and MDCK cell-monolayers A mechanistic model Bittermann,Kai; Goss,Kai-Uwe; Abstract.Publication PLoS ONE.Pub Date December 2017 DOI 10.1371/journal.pone.0190319 Bibcode 2017PLoSO..1290319B full text sources

Revisiting atenolol as a low passive permeability marker

Oct 31,2017 Predicting apparent passive permeability of Caco#0183;Atenolol is a selective beta receptor blocker for the treatment of hypertension with the enantiomer S-atenolol responsible for the main active pharmacological effect [1,2,3].For a long time,atenolol has been considered as a typical representative of a hydrophilic small molecule with low passive permeability and low paracellular diffusion across intestinal membrane and bloodbrain barrier (BBB).Relationship between Passive Permeability,Efflux,and Further analysis revealed that the accuracy of the prediction was differentiated by permeability and P-glycoprotein- (P-gp) and mouse breast cancer resistance protein (mBcrp)-mediated efflux.For proprietary compounds with passive permeability greater than 5 Predicting apparent passive permeability of Caco#215; 106 cm/s and efflux ratios less than 5 in both P-gp- and mBcrp-expressing cells Recent Advances in Computational Prediction of Drug retical models to predict drug absorption-related properties,such as intestinal absorption,Caco-2 permeability,and blood-brain partitioning are reviewed.The important physicochemical properties used in the prediction of drug absorp-tion,and the relevance of predictive models in the evaluation of passive drug absorption are discussed.

Recent Advances in Computational Prediction of Drug

retical models to predict drug absorption-related properties,such as intestinal absorption,Caco-2 permeability,and blood-brain partitioning are reviewed.The important physicochemical properties used in the prediction of drug absorp-tion,and the relevance of predictive models in the evaluation of passive drug absorption are discussed.QSAR Prediction of Passive Permeability in the LLCPK1 Mar 12,2012 Predicting apparent passive permeability of Caco#0183;The QSAR model was used to predict the Caco2 cell permeability for 313 compounds described in the literature with good success.We find that passive permeability for different cell lines can be predicted with similar molecular properties and descriptors.Prediction of Membrane Permeability to Peptides from Purpose.To develop a theoretical method for prediction of transcellular permeability to peptides.Methods.The dynamic molecular surface properties of 19 oligopeptide derivatives,divided into three homologous series were calculated.The dynamic molecular surface properties were compared with commonly used experimental predictors of membrane permeability such as partition coefficients.

Prediction of Membrane Permeability to Peptides from

Purpose.To develop a theoretical method for prediction of transcellular permeability to peptides.Methods.The dynamic molecular surface properties of 19 oligopeptide derivatives,divided into three homologous series were calculated.The dynamic molecular surface properties were compared with commonly used experimental predictors of membrane permeability such as partition coefficients.Prediction of Caco-2 pH-Dependent PermeabilityCaco-2 permeability profile took into account,transcellular passive (neutral and charged species),paracellular,aqueous boundary layer (ABL),and filter-limited permeability.Fig.2.Prediction of the intrinsic Caco-2 permeability,using intrinsic Double-Sink PAMPA permeability,calculated apparentPrediction Of Coefficient Of Permeability OfThe Caco-2 permeability screen is considered to be more representative of human absorption in vivo than PAMPA (parallel artificial membrane permeability assay).PAMPA solely provides a measure of passive diffusion whereas the Caco-2 model provides better prediction of the human absorption for compounds which display active uptake or efflux or

Predicting apparent passive permeability of Caco-2 and

Where P app (Caco-2/MDCK) is the apparent cell permeability through the Caco-2/MDCK cell monolayer at a pH of 7.4,P p a r a t o t a l is the permeability of the paracellular permeation pathway,P l a t e r a l t o t a l is the permeability of the lateral permeation pathway and P c y t o s o l i c t o t a l is the permeability of the cytosolic Predicting apparent passive permeability of Caco-2 and Predicting apparent passive permeability of Caco-2 and MDCK cell-monolayers A mechanistic model .By Kai Bittermann and Kai-Uwe Goss.Cite .BibTex; Full citation; Publisher Public Library of Science (PLoS) Year 2017.DOI identifier 10.1371/journal.pone.0190319.OAI identifier Provided by Predicting apparent passive permeability of Caco-2 and Dec 27,2017 Predicting apparent passive permeability of Caco#0183;The model seems to capture the most important permeability features.The prediction of log P app (Caco-2/MDCK,pH 7.4) with Eq (2) is satisfying (R 2 = 0.77,RMSE = 0.48),especially if one considers the high experimental uncertainty that becomes visible in the experimental scatter for single chemicals.Note that also some of the partitioning and diffusion parameters are modeled at different temperatures,which leads to additional uncertainty

Predicting Phenolic Acid Absorption in Caco-2 Cells A

There is a considerable need to rationalize the membrane permeability and mechanism of transport for potential nutraceuticals.The aim of this investigation was to develop a theoretical permeability equation,based on a reported descriptive absorption model,enabling calculation of the transcellular component of absorption across Caco-2 monolayers.Published data for Caco-2 permeability of 30 Passive diffusion of ciprofloxacin and its Mar 04,2021 Predicting apparent passive permeability of Caco#0183;Passive diffusion of ciprofloxacin and its metalloantibiotic a computational and experimental study it is classified as a low permeability substance in Caco-2 cell monolayers, is negligible at physiological conditions,we may predict that the permeability of the metalloantibiotic is larger than the one of the free drug.Conclusion.Modeling the pharmacodynamics of passive membrane permeabilityQikProp v3.2 was used to predict Caco-2 permeabilities .As QikProp does not predict PAMPA permeabilities,only Caco-2 permeabilities are reported.QikProp permeability calculations are conformationally invariant,and for both the FDA and congeneric set,starting conformations were used without minimization.

Intestinal permeability of the constituents from the roots

The bidirectional intestinal permeability of the active constituents from the roots of Saposhnikovia divaricata,including four coumarins,anomalin (1),5-methoxy-7-(3,3-dimethylallyloxy)coumarin (2),decursin (3),and decursinol angelate (4),as well as four chromones,cimifugin (5),prim-O-glucosyIntestinal absorption of S-nitrosothiols Permeability and The evaluation of the bidirectional apparent permeability demonstrated a passive diffusion of the three S-nitrosothiols.GSNO and NACNO preferentially cross the intestinal barrier though the transcellular pathway,while SNAP followed both the trans- and paracellular pathways.Influence of Passive Permeability on Apparent P Purpose.The objectives of this work were to evaluate the importance of moderate passive permeability on apparent P-glycoprotein (P-gp) kinetics,and demonstrate that inspection of basolateral to apical and apical to basolateral (BL-AP/AP-BL) permeability ratios may result in a compound being overlooked as a P-gp substrate and inhibitor of another drug's transport via P-gp inhibition.

How Well Can the Caco-2/MadinDarby Canine Kidney

The study aimed to predict effective human jejunal permeability (Peff) using a biophysical model based on parametrized paracellular,aqueous boundary layer,and transcellular permeabilities,and the villus-fold surface area expansion factor (kVF).Published human jejunal data (119 Peff,53 compounds) were analyzed by a regression procedure incorporating a dual-pore size paracellular model.HT29-MTX and Caco-2/TC7 monolayers as predictive models Abstract.The permeability of 19 compounds in both the Caco-2/TC7 and HT29-MTX models was determined,and the ability of each model to predict intestinal absorption in humans was compared.Similar apparent permeability values (log P(app)) were obtained in both models for the majority of compounds tested,and plots of log P(app) versus fraction absorbed in humans gave comparableEvaluation of Optimized Caco-2 PermeabilityThere are various contributions to passive transport of drugs through cell and basolateral aqueous boundary layers (P ABL (A) and P ABL (B)) barriers to drugs permeation in the cell-based (e.g.Caco-2) permeability assay.The apparent permeability coefficient Figure 2 demonstrates prediction of log permeability-pH profile for a weak base

Development of a Multicompartment PermeabilityLimited

Permeability data for a set of 28 compounds in Calu3 cells were collated from the literature.29-33 Permeability in Calu3 cells was also correlated to the in vitro permeability for the same set of compounds in Caco2 cells,25,34 so that Caco2 permeability can be used to predict Calu3 permeability.Determination of drug permeability and prediction ofAug 23,2007 Predicting apparent passive permeability of Caco#0183;Permeability coefcients across monolayers of the human colon carcinoma cell line Caco-2,cultured on permeable supports,are commonly used to predict the absorption of orally administered drugs Determination of drug permeability and prediction of drug Aug 23,2007 Predicting apparent passive permeability of Caco#0183;Permeability coefficients across monolayers of the human colon carcinoma cell line Caco-2,cultured on permeable supports,are commonly used to predict the absorption of orally administered drugs

Determination of drug absorption parameters in Caco-2

Prediction of in vivo absorption based on in vitro methodology may help reduce the volume of (e.g.passive permeability and active efflux) is still not the common procedure in the analysis of permeation data and the usually employed apparent permeability coefficient P app and efflux ratio (ER) are afflicted with limitations.The objective Determination and prediction of permeability across Jan 01,2020 Predicting apparent passive permeability of Caco#0183;It has been reported recently that Caco-2 permeability coefficients for 768 diverse drugs and druglike compounds could account for passive diffusion across the mucosal epithelium using a minimal set of physicochemical descriptors (octanolwater logD,pKa,hydrogen bonding potential,and molecular size),a model has been successfully set up to predict Caco-2 permeability coefficients .Current Projects - Helmholtz-Zentrum f Predicting apparent passive permeability of Caco#252;r UmweltforschungAlso,passive membrane permeability is a key to predicting uncoupling activity.Contact person at UFZ Andrea Ebert and Kai-Uwe Goss.References Bittermann,Kai,and Kai-Uwe Goss.2017.Predicting Apparent Passive Permeability of Caco-2 and MDCK Cell-Monolayers A Mechanistic Model. PLoS ONE 12(12) 120.

Comparative permeability of three saikosaponins and

Jun 30,2020 Predicting apparent passive permeability of Caco#0183;Bidirectional permeability of test compounds on Caco-2 cells was evaluated by apparent permeability coefficient (P app) calculated according to the following equation,single time point method was used in our experiment P app = (dC / dt) Predicting apparent passive permeability of Caco#215; V R / (A Predicting apparent passive permeability of Caco#215; C 0) where dC is the corresponding concentration of the test compound in the receiving compartment at the end time point of transport,dtCited by 17Publish Year 2017Author Kai Bittermann,Kai-Uwe Goss,Kai-Uwe GossPredicting apparent passive permeability of Caco-2 and Dec 27,2017 Predicting apparent passive permeability of Caco#0183;Experimentally derived apparent permeabilities,Papp,through cell monolayers such as Caco-2 and MDCK are considered to be an in-vitro gold standard for assessing the uptake efficiency of drugs.Here,we present a mechanistic model that describes 'passive' Papp values (i.e.,neglecting active transport) by accounting for the different resistances solutes encounter when permeating a cellCited by 17Publish Year 2017Author Kai Bittermann,Kai-Uwe Goss,Kai-Uwe GossPredicting Caco-2 Permeability Using Support Vector prediction model.RESULTS The correlation coefficients (r) of the experimental and predicted Caco-2 apparent permeability for the training set and the test set were 0.88 and 0.85,respectively.CONCLUSIONS The results suggest that the SVM method is effective for predicting Caco-2 permeability.Membrane permeability of

Cited by 17Publish Year 2017Author Kai Bittermann,Kai-Uwe Goss,Kai-Uwe GossPeople also askHow is Caco-2 permeability measured?How is Caco-2 permeability measured?A bi-directional Caco-2 permeability assay is performed where the transport of the compound is measured in the apical to basolateral direction as well as the basolateral to apical direction.The result is typically reported as an efflux ratio i.e.P app (B-A)/P app (A-B).Caco-2 Permeability Assay - CyprotexCited by 17Publish Year 2017Author Kai Bittermann,Kai-Uwe Goss,Kai-Uwe Goss Predicting apparent passive permeability of Caco-2

Experimentally derived apparent permeabilities,Papp,through cell monolayers such as Caco-2 and MDCK are considered to be an in-vitro gold standard for assessing the uptake efficiency of drugs.Here,we present a mechanistic model that describes passive Papp values (i.e.,neglecting active transport) by accounting for the different resistances solutes encounter when permeating a cell monolayer.Cell Permeability Efficacy - Creative BiolabsCaco-2 Permeability Assay The Caco-2 permeability assay utilizes Caco-2 cell line derived from human colon carcinoma.This cell line has many characteristics that resemble intestinal epithelial cells including the formation of a polarized monolayer,intercellular tight junctions and well-defined brush border on the apical surface.

Caco-2 Permeability Assay,In Vitro Drug Metabolism

Caco-2 Permeability Assay.Predict intestinal permeability and oral absorption of compounds.The Caco-2 monolayer is widely used across the pharmaceutical industry as an in vitro model of the human small intestinal mucosa to predict the absorption of orally administered drugs. Predicting apparent passive permeability of Caco#185;Caco-2 Permeability Assay - IONTOXPredict the intestinal permeability and oral absorption of your test compound using our Caco-2 permeability assay.The Caco-2 permeability assay is an FDA required assay for companies applying for an Investigational New Drug (IND) and delivers keyCaco-2 Permeability Assay - DDA PlatformCaco-2 permeability assay is a part of our portfolio of in vitro ADME screening services.Creative Bioarray delivers consistent,high quality Caco-2 assay data with cost-efficiency that comes from a highly automated approach.Available Caco-2 Permeability Assay at Creative Bioarray.Passive permeability in Caco-2; Evaluation of MDR1 substrate

Caco-2 Permeability Assay - Cyprotex

Cyprotex's Caco-2 permeability assay uses an established method that measures the rate of flux of a compound across polarised Caco-2 cell monolayers and from which the data generated can be used to predict in vivo absorption of drugs.The Caco-2 cell line is derived from a human colon carcinoma.Caco-2 Permeability - Creative BiolabsIn addition to determine the permeability by passive diffusion,Caco-2 cells can also assess the permeability by active uptake/efflux and paracellular active transport as they can express transporter proteins,efflux proteins,and Phase II conjugation enzymes.In many cases,the Caco-2 cell monolayer mimics the human intestinal epithelium.AID 299831 - Apparent permeability across human Caco-2 Title Caco-2 cell permeability and stability of two d-glucopyranuronamide conjugates of thyrotropin-releasing hormone.Abstract Caco-2 cell permeability and stability assays were used as an in vitro model to study the intestinal epithelial transport and stability of two analogues of thyrotropin-releasing hormone (TRH; Pyr-His-Pro-NH2).

ADME Properties Evaluation in Drug Discovery Prediction

The Caco-2 cell monolayer model is a popular surrogate in predicting the in vitro human intestinal permeability of a drug due to its morphological and functional similarity with human enterocytes.A-to-B B-to-A - Efflux - ratio Ncompounds in differentiated CACO-2 cultures in their ability to demonstrate these transport functions.There are several ways in which the permeability data can be used.Firstly,the compounds can be ranked in terms of their CACO-2 P app values.Two reference compounds,atenolol (paracellular transport) and propranolol (passive transcellularA General Model for Prediction of Caco2 Cell Permeability In order to deal with current issues of data quantity and quality the wellestablished Caco2 cell model was used to generate accurate permeability data of apparent passive transport for a large set of structurally diverse compounds.PLS statistics was used to correlate calculated descriptors to log P app.This new prediction model for Caco2 cell permeability has incorporated many different descriptor types to deal with the multivariate nature of permeability.

(PDF) Predicting apparent passive permeability of Caco-2

Dec 27,2017 Predicting apparent passive permeability of Caco#0183;Predicting apparent passive permeability of Caco-2 and MDCK cell-monolayers A mechanistic model(PDF) Comparison between active and passive drugPrediction of human active drug transport in Caco-2 monolayers will therefore only be possible after characterisation of each transport system and subsequent introduction of a scaling factor to compensate for the different expression of the carrier in Caco-2 cells from that seen in vivo.The human effective permeability coefficient (P~f0 is results for this questionWhat is Cyprotex's Caco-2 permeability?What is Cyprotex's Caco-2 permeability?Cyprotex's Caco-2 Permeability data can be used in conjunction with Cyprotex's Turbidimetric Solubility data to predict dose dependent human intestinal absorption.Please refer to our Human Intestinal Absorption Model section for further details.Caco-2 Permeability Assay - Cyprotex

results for this questionWhat is Caco 2 permeability assay?What is Caco 2 permeability assay?Caco-2 permeability assay to investigate intestinal permeability.Cyprotex's Caco-2 Permeability assay uses an established method for predicting the in vivo absorption of drugs across the gut wall by measuring the rate of transport of a compound across the Caco-2 cell line.The Caco-2 cell line is derived from a human colon carcinoma.Caco-2 Permeability Assay - Cyprotex results for this questionHow is the permeability coefficient calculated?How is the permeability coefficient calculated?The permeability coefficient (P app) is calculated from the following equation Where dQ/dt is the rate of permeation of the drug across the cells,C 0 is the donor concentration at time zero and A is the area of the cell monolayer.How do I interpret the data from the Caco-2 permeability assay?Caco-2 Permeability Assay - Cyprotex results for this questionFeedbackPredicting apparent passive permeability of Caco-2

app (Caco-2,pH 7.4) values which had efflux ratios of 2 or higher.For the remaining data,multiple P app (pH 7.4) values reported in one source,including P app (pH 7.4) values measured in both directions (apical to basolateral and basolat-eral to apical),were averaged.These,still cell line specific,passive apparent cell permeability

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