OC000459 is a potent, selective, and orally active D prostanoid receptor 2 antagonist that inhibits mast cell-dependent activation of T helper 2 lymphocytes and eosinophils. OC000459 inhibited chemotaxis (IC50 = 0.028 μM) of human Th2 lymphocytes and cytokine production (IC50 = 0.019 μM) by human Th2 lymphocytes. OC000459 also inhibited the activation of Th2 cells and eosinophils in response to supernatants from IgE/anti-IgE-activated human mast cells. OC000459 was shown to inhibit blood eosinophilia in rats induced by 13,14-dihydro-15-keto PGD2 (Item No. 12610) (ED50 = 0.04 mg/kg) and airway eosinophilia in guinea pigs in response to an aerosol of 13,14-dihydro-15-keto PGD2 (ED50 = 0.01 mg/kg). OC000459 treatment inhibited LAR and post-allergen increase in sputum eosinophils and led to a significant and persistent reduction in the symptoms of rhinoconjunctivitis.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
The CRTH2 antagonist OC000459 reduces nasal and ocular symptoms in allergic subjects exposed to grass pollen, a randomised, placebo-controlled, double-blind trial.
Horak F, et al. Allergy. 2012 Dec;67(12):1572-9. PMID: 23025511.
Inhibition of the asthmatic allergen challenge response by the CRTH2 antagonist OC000459.
Singh D, et al. Eur Respir J. 2013 Jan;41(1):46-52. PMID: 22496329.
Pharmacologic profile of OC000459, a potent, selective, and orally active D prostanoid receptor 2 antagonist that inhibits mast cell-dependent activation of T helper 2 lymphocytes and eosinophils.
Pettipher R, et al. J Pharmacol Exp Ther. 2012 Feb;340(2):473-82. PMID: 22106101.
A randomized, double-blind, placebo-controlled study of the CRTH2 antagonist OC000459 in moderate persistent asthma.
Barnes N, et al. Clin Exp Allergy. 2012 Jan;42(1):38-48. PMID: 21762224.
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