AMG 853

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Description: Potent dual CRTH2 and prostaglandin D2 (PGD2) receptor antagonist
Chemical Name: 5-Chloro-4-[2-[[(2-chloro-4-cyclopropylphenyl)sulfonyl]amino]-4-[[(1,1-dimethylethyl)amino]carbonyl]phenoxy]-2-fluorobenzeneacetic acid
Purity: ≥98% (HPLC)
Reviews (1)

Biological Activity for AMG 853

AMG 853 is a potent prostaglandin D2 (PGD2, CRTH2) receptor antagonist (IC50 values are 8 and 35 nM, respectively in plasma). Inhibits PGD2-induced down modulation of CRTH2 on CD16- granulocytes in human whole blood as well as PGD2-induced cAMP response in platelets. Inhibits PGD2-induced airway constriction in vivo. Orally bioavailable.

Technical Data for AMG 853

M. Wt 609.49
Formula C28H27Cl2FN2O6S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1169483-24-2
PubChem ID 42641863
Smiles ClC1=CC(C2CC2)=CC=C1S(NC3=CC(C(NC(C)(C)C)=O)=CC=C3OC4=C(Cl)C=C(CC(O)=O)C(F)=C4)(=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for AMG 853

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 60.95 100
ethanol 60.95 100

Preparing Stock Solutions for AMG 853

The following data is based on the product molecular weight 609.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.64 mL 8.2 mL 16.41 mL
5 mM 0.33 mL 1.64 mL 3.28 mL
10 mM 0.16 mL 0.82 mL 1.64 mL
50 mM 0.03 mL 0.16 mL 0.33 mL

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References for AMG 853

References are publications that support the biological activity of the product.

Liu et al (2011) Discovery of AMG 853, a CRTH2 and DP dual antagonist. ACS Med.Chem.Lett. 2 326 PMID: 24900313

If you know of a relevant reference for AMG 853, please let us know.

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Keywords: AMG 853, AMG 853 supplier, AMG853, CRTH2, chemoattractant, receptor-homologous, molecule, expressed, on, Th2, cells, PGD2, prostaglandin, receptor, dual, antagonists, antagonism, orally, DP2, bioavailable, Prostanoid, Receptors, 5701, Tocris Bioscience

Citations for AMG 853

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Reviews for AMG 853

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AMG 853 blocks p38 phosphorylation in 15d-PGJ2 treated cardiomyocytes.
By Chintan Koyani on 12/10/2018
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: HL-1 cardiomyocytes

HL-1 cardiomyocytes were pre-incubated with AMG 853 (1 µM, 30 min) followed by treatment with 15d-PGJ2 (15 µM, 30 min) to follow p38 activation using Western blot analysis. AMG 853 inhibited 15d-induced p38 phosphorylation.

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