Potent dual CRTH2 and prostaglandin D2 (PGD2) 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. Also inhibits BRD4 (Kd = 170 nM). Orally bioavailable.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 609.49. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|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|
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
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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, bioavailable, Prostanoid, Receptors, 5701, Tocris Bioscience
Citations for AMG 853
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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.
Literature in this Area
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.