Golgicide A

Modify Date: 2023-01-15 12:48:45

Golgicide A structure	Common Name	Golgicide A
	CAS Number	853138-65-5	Molecular Weight	439.54900
	Density	1.217g/cm3	Boiling Point	704.6ºC at 760 mmHg
	Molecular Formula	C₂₈H₂₉N₃O₂	Melting Point	N/A
	MSDS	Chinese USA	Flash Point	379.9ºC
	Symbol	GHS07	Signal Word	Warning

Use of Golgicide A

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].

Name	2-[[2-(1H-indol-3-yl)acetyl]-methylamino]-2-phenyl-N-(4-propan-2-ylphenyl)acetamide
Synonym	More Synonyms

Description	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].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> CFTR Research Areas >> Endocrinology
Target	CFTR[1]
In Vitro	PG01 itself does not activate ∆F508-CFTR, produces substantial ∆F508-CFTR Cl- current after the addition of 0.5 and 2 μM Forskolin. PG01 at 100 nM strongly stimulates channel activity with multiple channel openings observed. The apparent Kd for PG01 for G551D-CFTR activation is 1 μM, approximately 100-fold better than that of genistein. The potency for activation G1349D-CFTR by PG01 is even better at 40 nM. PG01 produces large currents in both G551D- and G1349D-CFTR expressing cells. The currents are sensitive to CFTRinh-172 and are not seen in nontransfected cells[1].
In Vivo	Pharmacokinetic analysis of PG01 in rats is done by serial measurements of plasma concentrations after single bolus infusions (5 mg/kg). PG01 pharmacokinetics fitted a two-compartment model with half-times of ＜5 min and 130 min with volume of distribution 4 L. Microsome metabolism studies and rat pharmacokinetic analysis suggests significantly more rapid metabolism of PG01 than SF-03[1].
References	[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.

Density	1.217g/cm3
Boiling Point	704.6ºC at 760 mmHg
Molecular Formula	C₂₈H₂₉N₃O₂
Molecular Weight	439.54900
Flash Point	379.9ºC
Exact Mass	439.22600
PSA	65.20000
LogP	5.74520
Index of Refraction	1.662

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302-H413
Hazard Codes	Xn
RIDADR	NONH for all modes of transport

PG-01

Phenylglycine-01

DC Chemicals Limited
China
Product Name: PG01
Price:
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: PHENYLGLYCINE-01
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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Golgicide A

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