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Submit ReviewAMG 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.
M. Wt | 609.49 |
Formula | C28H27Cl2FN2O6S |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 1169483-24-2 |
PubChem ID | 42641863 |
InChI Key | PFWVGKROPKKEDW-UHFFFAOYSA-N |
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 60.95 | 100 | |
ethanol | 60.95 | 100 |
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.
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
If you know of a relevant reference for AMG 853, please let us know.
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
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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.