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PG01

Catalog No. T16516 CAS 853138-65-5

Synonyms: Phenylglycine-01

PG01 is a potent CFTR Cl-channel potentiator, effective against ΔF508 (Ka 0.3 μM), and also against E193K, G970R and G551D (CFTR mutants), with Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively.PG01 increases ΔF508-CFTR Cl- currents upon addition of forskolin. F508-CFTR Cl-current upon addition of Forskolin, correcting the gating defect of CFTR mutants.

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PG01, CAS 853138-65-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 126.00
5 mg	In stock	$ 378.00
10 mg	In stock	$ 568.00
25 mg	In stock	$ 913.00
50 mg	In stock	$ 1,230.00
100 mg	In stock	$ 1,680.00
500 mg	In stock	$ 3,360.00
1 mL * 10 mM (in DMSO)	In stock	$ 368.00

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Purity: 99.87%

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Description	PG01 is a potent CFTR Cl-channel potentiator, effective against ΔF508 (Ka 0.3 μM), and also against E193K, G970R and G551D (CFTR mutants), with Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively.PG01 increases ΔF508-CFTR Cl- currents upon addition of forskolin. F508-CFTR Cl-current upon addition of Forskolin, correcting the gating defect of CFTR mutants.
Targets&IC50	E193K:0.22 μM(Kd), G970R:0.45 μM(Kd), CFTR (G551D):1.94 μM(Kd)
In vitro	PG01 induces significant currents in cells expressing either G551D- or G1349D-CFTR. While PG01 alone does not activate ∆F508-CFTR, it notably enhances ∆F508-CFTR Cl- current in the presence of Forskolin (0.5 and 2 μM). At a concentration of 100 nM, PG01 markedly increases channel activity, evidenced by frequent channel openings. The compound's effectiveness in activating G551D-CFTR, with an apparent Kd of 1 μM, is roughly 100 times greater than that of genistein, and its potency in activating G1349D-CFTR is superior, requiring only 40 nM. These currents are blocked by CFTRinh-172 and absent in nontransfected cells, indicating specificity for CFTR modulation.[1]
In vivo	Microsome metabolism studies and rat pharmacokinetic analysis indicate that PG01 metabolizes significantly faster than SF-03. The pharmacokinetics of PG01 in rats were assessed through serial plasma concentration measurements following single bolus infusions (5 mg/kg), revealing that its pharmacokinetics adhere to a two-compartment model with elimination half-times of less than 5 minutes and 130 minutes, and a distribution volume of 4 L.[1]

Synonyms	Phenylglycine-01
Molecular Weight	439.55
Formula	C28H29N3O2
CAS No.	853138-65-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (68.25 mM)

References and Literature

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. 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.

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This product is contained In the following compound libraries：

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Keywords

PG01 853138-65-5 Membrane transporter/Ion channel CFTR PG 01 PG-01 Phenylglycine-01 inhibitor inhibit

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