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Submit ReviewCystic fibrosis transmembrane conductance regulator (CFTR) potentiator. Corrects gating defects of CFTR mutants such as ΔF508 (Ka = 0.3 μM), E193K and G970R (Kd values are 0.22 μM and 0.45 μM respectively). Increases ΔF508-CFTR Cl- currents in the presence of forskolin; displays no effect on Ca2+-activated Cl- current.
分子量 | 439.55 |
公式 | C28H29N3O2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 853138-65-5 |
PubChem ID | 4695397 |
InChI Key | PQAYCXMQTUEDRD-UHFFFAOYSA-N |
Smiles | O=C(C(C2=CC=CC=C2)N(C)C(CC3=CNC4=C3C=CC=C4)=O)NC1=CC=C(C(C)C)C=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Pedemonte et al (2005) Phenylglycine and sulphonamide correctors of defective DF508 and G551D cystic fibrosis transmembrane conductance regulator chloride-channel gating. Mol.Pharmacol. 67 1797 PMID: 15722457
Caputo et al (2009) Mutation-specific potency and efficacy of cystic fibrosis transmembrane conductance regulator chloride channel potentiators. J.Pharmacol.Exp.Ther. 330 783 PMID: 19491324
Pedemonte et al (2010) Influence of cell background on pharmacological rescue of mutant CFTR. Am.J.Physiol.Cell Physiol 298 C866 PMID: 20053923
关键词: PG 01, PG 01 supplier, PG01, CTFR, mutant, potentiators, cystic, fibrosis, transmembrane, conductance, channels, CFTR, chloride, Cl-, pharmacochaperones, 3943, Tocris Bioscience
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