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OC000459

Cat. No. M2091

OC000459 Structure
Size Price Availability Quantity
10mg USD 140 In stock
50mg USD 480 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 348.37
Formula C21H17FN2O2
CAS Number 851723-84-7
Purity >99%
Solubility DMSO
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




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