PGD97
PGD97 is a selective cyclic peptide inhibitor against CAL/CFTR interactions, with a KD 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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 2717490-36-1
- Formel: C74H111N23O14S3
- Molecular Weight:1643.01
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
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.
Chemical Information
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CAS. Nr. 2717490-36-1
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Molecular Weight 1643.01
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Formel C74H111N23O14S3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)