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AMG-009

Catalog No. T14211 CAS 1027847-67-1

AMG-009 is a prostaglandin D2 antagonist. For CRTH2 and DP receptors, the IC50s are 3 nM and 12 nM, respectively.

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AMG-009, CAS 1027847-67-1

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

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Description	AMG-009 is a prostaglandin D2 antagonist. For CRTH2 and DP receptors, the IC50s are 3 nM and 12 nM, respectively.
Targets&IC50	CRTH2/DP2 receptor:3 nM
In vitro	AMG 009 inhibits guinea pig CRTH2 receptors (IC50=3 nM) and a PGD2-induced cAMP response assay with cells expressing the guinea pig DP receptors (Ki=131 nM)[1]. AMG-009 inhibits PGD2-induced down-modulation of CRTH2 on CD16 negative granulocytes (eosinophils) in human whole blood with a Ki of 1 nM and it also inhibits PGD2-induced cAMP response mediated by DP in platelets in 80% human whole blood with a Ki of 148 nM.
In vivo	AMG 009 (3, 10 or 30 mg/kg, s.c.) results in a dose dependent decrease in airway resistance provoked by PGD2 aerosol in an acute guinea pig model[1]. AMG 009 significantly improves DP potency, with Kb of 82 nM, in a guinea pig model of PGD2-induced airway constriction[2].

Molecular Weight	581.46
Formula	C26H26Cl2N2O7S
CAS No.	1027847-67-1

Storage

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

References and Literature

1. Liu J, et al. Discovery and optimization of CRTH2 and DP dual antagonists. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6419-23. 2. Liu J, et al. Discovery of AMG 853, a CRTH2 and DP Dual Antagonist. ACS Med Chem Lett. 2011 Mar 2;2(5):326-30. 3. Johnson MG, et al. Solving time-dependent CYP3A4 inhibition for a series of indole-phenylacetic acid dual antagonists of the PGD(2) receptors CRTH2 and DP. Bioorg Med Chem Lett. 2014 Jul 1;24(13):2877-80.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

AMG-009 1027847-67-1 Others AMG009 AMG 009 inhibitor inhibit

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