| Description | Vidupiprant (AMG 853) is an effective dual antagonist of CRTH2 and prostanoid D receptor with IC50s of 8 nM and 35 nM in human plasma. Vidupiprant can be used in studies about the treatment of asthma. |
| In vitro | Vidupiprant inhibits prostaglandin D2-induced cAMP response in platelets in 80% human whole blood with a Kb of 4.7 nM. Vidupiprant inhibits the prostaglandin D2 -induced down-modulation of CRTH2 on CD16 negative granulocytes in human whole blood with a Kb of 0.2 nM. Vidupiprant demonstrates antagonist activity in an aequorin assay using CRTH2-transfected HEK 293 cells and an eosinophil shape change assay[1]. |
| In vivo | In a guinea pig model of PGD2-induced airway constriction, airway resistance is measured in response to PGD2 challenge. Vidupiprant has a Kb of 5 nM[1]. |
| Synonyms | AMG 853 |
| molecular weight | 609.49 |
| Molecular formula | C28H27Cl2FN2O6S |
| CAS | 1169483-24-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 95 mg/mL (155.87 mM), Sonication is recommended. |
| References | 1. 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. |