Source Name: 2015_Hewitt

Literature Information

Literature Title Cell-permeable cyclic peptides from synthetic libraries inspired by natural products
Doi 10.1021/ja508766b
Research Group
  1. Department of Chemistry and Biochemistry, University of California Santa Cruz
  2. Department of Pharmaceutical Chemistry, University of California San Francisco
  3. Department of Antibody Discovery & Protein Engineering, Medimmune Ltd.
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Data Number 18
Minimum Molecular Weight 712.9
Maximum Molecular Weight 755.0


Assay Information 1

Assay Type Caco2
Permeability Type logPe
Membrane Measurement Direction (Exclude PAMPA) Apical to Basolateral (AB)
Assay Detail Analysis of all individually synthesized compounds by the established Caco-2 assay was outsourced to Cyprotex. For specific details of the assay conditions, interested parties should contact Cyprotex directly. In general, after a 20Aday cell culture of Caco-2 cells, individual compounds were were incubated at 10 µM for 2 h and 37 °C, after which concentrations in apical and basolateral compartments were quantified by LCAMS/MS to calculate compound flux in AAtoAB direction. Lucifer Yellow was used to validate membrane integrity of the Caco-2 cell monolayer and Atenolol, Propranolol, and Talinolol were used as controls with known Caco-2 permeability.


Assay Information 2

Assay Type -
Permeability Type -
Membrane Measurement Direction (Exclude PAMPA) -
Assay Detail -