AMG-009

Name: AMG-009
Brand: MedChemExpress
SKU: HY-19499
Rating: 4.5 (1 reviews)

Cat. No.: HY-19499 Purity: 98.08%: FAQs
Data Sheet SDS COA Handling Instructions

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AMG-009 is a potent antagonist of prostaglandin D2, with IC₅₀ of 3 nM and 12 nM for CRTH2 and DP receptors, respectively.

For research use only. We do not sell to patients.

AMG-009 Chemical Structure

CAS No. : 1027847-67-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 192	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 192	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 470	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1100	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

AMG-009 is a potent antagonist of prostaglandin D2, with IC₅₀ of 3 nM and 12 nM for CRTH2 and DP receptors, respectively.

IC₅₀ & Target^[3]

12 nM (IC₅₀)

CRTH2

3 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.003 μM Compound: AMG-009	Displacement of [3H]PGD2 from human CRTH2 receptor expressed in 293 cells by scintillation counting in presence of 0.5 % BSA Displacement of [3H]PGD2 from human CRTH2 receptor expressed in 293 cells by scintillation counting in presence of 0.5 % BSA	[PMID: 22119474]
HEK293	IC₅₀	0.003 μM Compound: 31, AMG-009	Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK 293 cells in presence of 0.5% BSA by scintillation counting Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK 293 cells in presence of 0.5% BSA by scintillation counting	[PMID: 19804971]
HEK293	IC₅₀	0.003 μM Compound: 1, AMG-009	Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin	[PMID: 24900313]
HEK293	IC₅₀	0.012 μM Compound: AMG-009	Displacement of [3H]PGD2 from human DP receptor expressed in 293 cells by scintillation counting in presence of 0.5 % BSA Displacement of [3H]PGD2 from human DP receptor expressed in 293 cells by scintillation counting in presence of 0.5 % BSA	[PMID: 22119474]
HEK293	IC₅₀	0.012 μM Compound: 31, AMG-009	Displacement of [3H]-PGD2 from human DP receptor expressed in HEK 293 cells in presence of 0.5% BSA by scintillation counting Displacement of [3H]-PGD2 from human DP receptor expressed in HEK 293 cells in presence of 0.5% BSA by scintillation counting	[PMID: 19804971]
HEK293	IC₅₀	0.012 μM Compound: 1, AMG-009	Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin	[PMID: 24900313]
HEK293	IC₅₀	0.021 μM Compound: AMG-009	Displacement of [3H]PGD2 from human CRTH2 receptor expressed in HEK293 cells by scintillation counting in presence of 50% plasma Displacement of [3H]PGD2 from human CRTH2 receptor expressed in HEK293 cells by scintillation counting in presence of 50% plasma	[PMID: 22264478]
HEK293	IC₅₀	0.021 μM Compound: AMG-009	Displacement of [3H]PGD2 from human CRTh2 receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma Displacement of [3H]PGD2 from human CRTh2 receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma	[PMID: 22119474]
HEK293	IC₅₀	0.021 μM Compound: 1, AMG-009	Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma	[PMID: 24900313]
HEK293	IC₅₀	0.28 μM Compound: AMG-009	Displacement of [3H]PGD2 from human DP receptor expressed in HEK293 cells by scintillation counting in presence of 50% plasma Displacement of [3H]PGD2 from human DP receptor expressed in HEK293 cells by scintillation counting in presence of 50% plasma	[PMID: 22264478]
HEK293	IC₅₀	0.28 μM Compound: AMG-009	Displacement of [3H]PGD2 from human DP receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma Displacement of [3H]PGD2 from human DP receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma	[PMID: 22119474]
HEK293	IC₅₀	0.28 μM Compound: 1, AMG-009	Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma	[PMID: 24900313]
HEK293	IC₅₀	12 nM Compound: AMG 009	Displacement of [3H]-PGD2 from human DP receptor expressed in HEK293 cells in buffer solution with 0.5% bovine serum albumin by scintillation counting Displacement of [3H]-PGD2 from human DP receptor expressed in HEK293 cells in buffer solution with 0.5% bovine serum albumin by scintillation counting	[PMID: 24825301]
HEK293	IC₅₀	3 nM Compound: AMG 009	Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK293 cells in buffer solution with 0.5% bovine serum albumin by scintillation counting Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK293 cells in buffer solution with 0.5% bovine serum albumin by scintillation counting	[PMID: 24825301]

In Vitro

AMG-009 inhibits PGD2-induced down-modulation of CRTH2 on CD16 negative granulocytes (eosinophils) in human whole blood with a K_i of 1 nM. AMG 009 also inhibits PGD2-induced cAMP response mediated by DP in platelets in 80% human whole blood with a K_i of 148 nM. 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 (K_i=131 nM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]. In a guinea pig model of PGD2-induced airway constriction, AMG 009 significantly improves DP potency, with K_b of 82 nM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

581.46

Formula

C₂₆H₂₆Cl₂N₂O₇S

CAS No.

1027847-67-1

Appearance

Solid

Color

White to light brown

SMILES

O=C(O)CC1=CC=C(OC2=CC=C(C(NCCCC)=O)C=C2NS(=O)(C3=CC=C(Cl)C=C3Cl)=O)C(OC)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (214.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7198 mL	8.5990 mL	17.1981 mL
5 mM	0.3440 mL	1.7198 mL	3.4396 mL
10 mM	0.1720 mL	0.8599 mL	1.7198 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.08%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

COA (251 KB) HNMR (299 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7198 mL	8.5990 mL	17.1981 mL	42.9952 mL
	5 mM	0.3440 mL	1.7198 mL	3.4396 mL	8.5990 mL
	10 mM	0.1720 mL	0.8599 mL	1.7198 mL	4.2995 mL
	15 mM	0.1147 mL	0.5733 mL	1.1465 mL	2.8663 mL
	20 mM	0.0860 mL	0.4300 mL	0.8599 mL	2.1498 mL
	25 mM	0.0688 mL	0.3440 mL	0.6879 mL	1.7198 mL
	30 mM	0.0573 mL	0.2866 mL	0.5733 mL	1.4332 mL
	40 mM	0.0430 mL	0.2150 mL	0.4300 mL	1.0749 mL
	50 mM	0.0344 mL	0.1720 mL	0.3440 mL	0.8599 mL
	60 mM	0.0287 mL	0.1433 mL	0.2866 mL	0.7166 mL
	80 mM	0.0215 mL	0.1075 mL	0.2150 mL	0.5374 mL
	100 mM	0.0172 mL	0.0860 mL	0.1720 mL	0.4300 mL

AMG-009 Related Classifications

Inflammation/Immunology Endocrinology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AMG-0091027847-67-1AMG009AMG 009Prostaglandin ReceptorInhibitorinhibitorinhibit

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AMG-009

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