Art. -Nr.: HY-19499

AMG-009

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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.

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Reinheit: 98.08%
CAS. Nr.: 1027847-67-1
Formel: C₂₆H₂₆Cl₂N₂O₇S
Molecular Weight:581.46

Speicherung:

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

AMG-009 Chemical Structure

CAS. Nr.: 1027847-67-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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)

Alle Prostaglandin Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
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	0.003 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: 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	0.012 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	0.012 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: 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	0.021 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	0.021 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: 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	0.28 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	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: 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	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]
HEK293	IC₅₀	3 nM Compound: 31, AMG-009	Displacement of [3H]-PGD2 from guinea pig CRTH2 receptor expressed in HEK293 cells Displacement of [3H]-PGD2 from guinea pig CRTH2 receptor expressed in HEK293 cells	[PMID: 19804971]
HEK293-EBNA	IC₅₀	30 μM Compound: 31, AMG-009	Displacement of [3H]SQ29548 from human TP receptor transfected in HEK 293 EBNA cells Displacement of [3H]SQ29548 from human TP receptor transfected in HEK 293 EBNA cells	[PMID: 19804971]

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.

Chemical Information

CAS. Nr. 1027847-67-1
Appearance Solid
Molecular Weight 581.46
Formel C₂₆H₂₆Cl₂N₂O₇S
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

Keywords

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AMG-009

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Endocrinology Compound Library

Angiogenesis-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle Prostaglandin Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AMG-009

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Endocrinology Compound Library

Angiogenesis-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle Prostaglandin Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AMG-009 Related Classifications

HY-19499 Related Classifications