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AG 045572

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Purity:98.99%

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COA HPLC HNMR

AG 045572

Catalog No. T22025Cas No. 263847-55-8

AG 045572 is a potent GnRH receptor antagonist that inhibits the GnRH receptor in humans and rats with Ki values of 6.0 nM and 3.8 nM, respectively.AG 045572 is metabolized by CYP3A and inhibits testosterone.

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Pack Size	Price	Availability
1 mg	$157	In Stock
5 mg	$268	In Stock
10 mg	$347	In Stock
25 mg	$595	In Stock
50 mg	$849	In Stock
100 mg	$1,170	In Stock
500 mg	$2,330	In Stock

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Product Introduction

Bioactivity

Description	AG 045572 is a potent GnRH receptor antagonist that inhibits the GnRH receptor in humans and rats with Ki values of 6.0 nM and 3.8 nM, respectively.AG 045572 is metabolized by CYP3A and inhibits testosterone.
In vitro	AG 045572 (10 μM, 40 min, for human liver microsomes; 10 μM, 10 min, for male rat liver microsomes; 1 μM, 10 min, for female rat liver microsomes) is metabolized by CYP3A in both rats and humans. The Km values in male and female human and female rat liver microsomes and expressed CYP3A4 and CYP3A5 were similar (0.39, 0.27, 0.28, 0.25, and 0.26 μM, respectively), while the Km values in male rat liver microsomes were 1.5 μM, indicating that AG-045572 is metabolized by different CYP3A isoenzymes in male and female rats.[1]
In vivo	AG 045572 (10 mg/kg (i.v.) or 20 mg/kg (p.o.), one time) in intact male rats showed moderate T1/2, CL and Vss but low oral bioavailability, with The bioavailability is higher in female rats (24%), and the pharmacokinetics in castrated male rats are similar to those in female rats.[1] The pharmacokinetics of AG 045572 (40 mg/kg; i.m.; twice a day for 3 days) in intact male rats changed, and the parameters were similar to those in female and castrated male rats.[1]

Chemical Properties

Molecular Weight	491.62
Formula	C30H37NO5
Cas No.	263847-55-8

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 55 mg/mL (111.88 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0341 mL	10.1705 mL	20.3409 mL	101.7046 mL
5 mM	0.4068 mL	2.0341 mL	4.0682 mL	20.3409 mL
10 mM	0.2034 mL	1.0170 mL	2.0341 mL	10.1705 mL
20 mM	0.1017 mL	0.5085 mL	1.0170 mL	5.0852 mL
50 mM	0.0407 mL	0.2034 mL	0.4068 mL	2.0341 mL
100 mM	0.0203 mL	0.1017 mL	0.2034 mL	1.0170 mL

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