PGD97 

PGD97 is a selective cyclic peptide inhibitor against CAL/CFTR interactions, with a K_D value of 6 nM towards the CAL PDZ domain for its desulfide cyclized form. PGD97 (desulfide cyclized form) has selectivity ≥ 130-fold compared to NHERF1/2 PDZ domains. PGD97 is capable of stabilizing F508del-CFTR at the cell membrane and improving CFTR function required for proper fluid homeostasis in tne lung. PGD97 can be used for the research of cystic fibrosis^[1].

PGD97 (Compound 24c) shows robust cellular entry efficiency into HeLa cells (61% relative to that of CPP9)^[1].
PGD97 (24 h, 37 °C) is highly stable in human serum, with ∼77% of the peptide remaining intact^[1].
PGD97 (5 μM) efficiently enters the membranes of HCT116 cells and is rapidly converted to a biologically active linear form by intracellular thiols (24), followed by partial degradation within the cell membrane^[1].
PGD97 (0-50 μM, 72 h) shows no significant cytotoxicity against cell lines (CFBE41o-, HCT116 and H358 cells) ^[1].
PGD97 (100 nM) increases shortcircuit currents by ∼3-fold and further potentiated the therapeutic effects of small-molecule correctors (e.g., VX-661) by ∼2-fold (with an EC₅₀ of ∼10 nM) in patient-derived F508del homozygous cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1643.01

C₇₄H₁₁₁N₂₃O₁₄S₃

2717490-36-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Dougherty PG, et al. Cyclic Peptidyl Inhibitors against CAL/CFTR Interaction for Treatment of Cystic Fibrosis. J Med Chem. 2020, 63(24):15773-15784.  [Content Brief]