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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2717490-36-1
- 分子式: C74H111N23O14S3
- 分子量:1643.01
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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.
化学情報
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CAS 番号 2717490-36-1
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分子量 1643.01
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分子式 C74H111N23O14S3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)