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Cat. No.: HY-P10226

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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.

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CAS No.: 2717490-36-1
Formule: C₇₄H₁₁₁N₂₃O₁₄S₃
Masse moléculaire:1643.01

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

PGD97 Chemical Structure

CAS No.: 2717490-36-1

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- In Vitro
Chemical Information
Pureté et documentation
Références
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Activité biologique

Description

In Vitro

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

CAS No. 2717490-36-1
Masse moléculaire 1643.01
Formule C₇₄H₁₁₁N₂₃O₁₄S₃
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (258 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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