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OC000459

Cat. No. M2091
OC000459 Structure
Synonym:

Timapiprant

Size Price Availability Quantity
10mg USD 132  USD132 In stock
50mg USD 350  USD350 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 348.37
Formula C21H17FN2O2
CAS Number 851723-84-7
Solubility (25°C) DMSO 4 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Horak F, et al. Allergy. The CRTH2 antagonist OC000459 reduces nasal and ocular symptoms in allergic subjects exposed to grass pollen, a randomised, placebo-controlled, double-blind trial.

[2] Singh D, et al. Eur Respir J. Inhibition of the asthmatic allergen challenge response by the CRTH2 antagonist OC000459.

[3] Pettipher R, et al. J Pharmacol Exp Ther. 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.

[4] Barnes N, et al. Clin Exp Allergy. A randomized, double-blind, placebo-controlled study of the CRTH2 antagonist OC000459 in moderate persistent asthma.

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Keywords: OC000459, Timapiprant supplier, GPR/FFAR, inhibitors, activators


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