Timapiprant

SKU: orb1223032

Description

Timapiprant, also known as OC000459, is a potent, selective and orally active CRTH2 antagonist. OC000459 reduces nasal and ocular symptoms in allergic subjects exposed to grass pollen, a randomised, placebo-controlled, double-blind trial. OC000459 inhibits mast cell-dependent activation of T helper 2 lymphocytes and eosinophils. OC000459 treatment inhibited LAR and post-allergen increase in sputum eosinophils. OC000459 appears to inhibit allergic inflammation in asthma.(In Vitro):Timapiprant (OC000459) (0.0001 μM-10 μM; 5 hours) inhibits chemotaxis (IC50=0.028 μM) of human Th2 lymphocytes and cytokine production (IC50=0.019 μM) by human Th2 lymphocytes.Timapiprant (OC000459) (1 μM) inhibits the activation of Th2 cells and eosinophils in response to supernatants from IgE/anti-IgE-activated human mast cells.Timapiprant (OC000459) (1 nM–1000 nM; 16 hours) inhibits the anti-apoptotic effect of PGD2 on Th2 cells with an IC50 of 0.035 uM.(In Vivo):Timapiprant (OC000459) (gavage; 2 mg/kg, 10 mg/kg) inhibits blood eosinophilia induced by 13,14-dihydro-15-keto-PGD2 (DK-PGD2) in Rat (ED50=0.04 mg/kg).Timapiprant (OC000459) (gavage; 0.01 mg/kg, 0.1 mg/kg, 1.0 mg/kg) inhibits airway eosinophilia in response to an aerosol of DK-PGD2 in guinea pigs (ED50=0.01 mg/kg).

Key Properties

• CAS Number: 851723-84-7
• MW: 348.37
• Purity: >98% (HPLC)
• Formula: C₂₁H₁₇FN₂O₂
• SMILES: Cc1c(Cc2nc3ccccc3cc2)c2c(ccc(F)c2)n1CC(=O)O
• Target: Norepinephrine
• Solubility: DMSO : 4 mg/mL 11.48 mM; H2O : < 0.1 mg/mL

Bioactivity

• In Vivo:
  Timapiprant (OC000459) (gavage; 2 mg/kg, 10 mg/kg) inhibits blood eosinophilia induced by 13, 14-dihydro-15-keto-PGD2 (DK-PGD2) in Rat (ED50 = 0.04 mg/kg). Timapiprant (OC000459) (gavage; 0.01 mg/kg, 0.1 mg/kg, 1.0 mg/kg) inhibits airway eosinophilia in response to an aerosol of DK-PGD2 in guinea pigs (ED50 = 0.01 mg/kg).
• In Vitro:
  Timapiprant (OC000459) (0.0001 μM-10 μM; 5 hours) inhibits chemotaxis (IC50 = 0.028 μM) of human Th2 lymphocytes and cytokine production (IC50 = 0.019 μM) by human Th2 lymphocytes. Timapiprant (OC000459) (1 μM) inhibits the activation of Th2 cells and eosinophils in response to supernatants from IgE/anti-IgE-activated human mast cells. Timapiprant (OC000459) (1 nM-1000 nM; 16 hours) inhibits the anti-apoptotic effect of PGD2 on Th2 cells with an IC50 of 0.035 uM. Apoptosis Analysis Cell line: Th2 Cells. Concentration: 0.0001 μM-10 μM Incubation time: 16 hours. Result: Inhibited the antiapoptotic effect of PGD2.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

OC000459 | OC-000459 | OC 000459 | Timapiprant

Quick Database Links

Gene Symbol

Norepinephrine