853138-65-5
Chemical Structure
PG01
- CAS No.: 853138-65-5
- Formula:C28H29N3O2
- Molecular Weight:439.55
IUPAC Name: 2-(2-(1H-indol-3-yl)-N-methylacetamido)-N-(4-isopropylphenyl)-2-phenylacetamide
InChIKey: PQAYCXMQTUEDRD-UHFFFAOYSA-N
SMILES: O=C(N(C)C(C1=CC=CC=C1)C(NC2=CC=C(C(C)C)C=C2)=O)CC3=CNC4=C3C=CC=C4
Biological Activity: PG01 is a potent CFTR Cl- channel potentiator. PG01 can correct gating defects of CFTR mutants, is effective on b>E193K, G970R and G551D (CFTR mutants) with Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively. PG01 is also effective on ΔF508 (Ka of 0.3 μM). PG01 increases ΔF508-CFTR Cl- current after adding Forskolin[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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PG01 | 98.04% | PG01 is a potent CFTR Cl- channel potentiator. PG01 can correct gating defects of CFTR mutants, is effective on b>E193K, G970R and G551D (CFTR mutants) with Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively. PG01 is also effective on ΔF508 (Ka of 0.3 μM). PG01 increases ΔF508-CFTR Cl- current after adding Forskolin. | ||||||||||||||||||||
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- [1]. Pedemonte N, et al. Phenylglycine and sulfonamide correctors of defective delta F508 and G551D cystic fibrosis transmembrane conductance regulator chloride-channel gating. Mol Pharmacol. 2005 May;67(5):1797-807. [Content Brief]
- [2]. Caputo A, et al. Mutation-specific potency and efficacy of cystic fibrosis transmembrane conductance regulator chloride channel potentiators. J Pharmacol Exp Ther. 2009 Sep;330(3):783-91. [Content Brief]
Keywords
