| Bioactivity | 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[1]. |
| Invitro | PGD97 (Compound 24c) 在 HeLa 细胞中显示出强的细胞进入效率 (相对于 CPP9 为 61) [1]。PGD97 (24 h，37 °C) 在人体血清中高度稳定，其中 ∼ 77% 的肽保持完整无损[1]。PGD97 (5 μM) 能有效进入 HCT116 细胞的细胞膜，并被细胞内的硫醇迅速还原成具有生物活性的线性形式 (24)，随后在细胞膜内发生部分降解[1]。PGD97 (0-50 μM，72 h) 对细胞系 CFBE41o-、HCT116 和 H358 都无明显的细胞毒性[1]。PGD97 (100 nM) 可使患者来源的 F508del 基因同源细胞中的短路电流增加 ∼ 3 倍，并使小分子校正剂 (如 VX-661) 的治疗效果进一步增强 ∼2 倍 (∼ 10 nM 的 EC50)[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PGD97 相关抗体: |
| CAS | 2717490-36-1 |
| Formula | C74H111N23O14S3 |
| Molar Mass | 1643.01 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
PGD97
CAS: 2717490-36-1 F: C74H111N23O14S3 W: 1643.01
PGD97 is a selective cyclic peptide inhibitor against CAL/CFTR interactions, with a KD value of 6 nM towards the CAL PDZ
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.