Timapiprant

• Description:

  Timapiprant (OC000459) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant (OC000459) potently displaces [3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM) . Timapiprant (OC000459) inhibits mast cell activation of Th2 lymphocytes and eosinophils[1].

• Product Name Alternative:

  OC000459

• UNSPSC:

  12352005

• Target:

  Prostaglandin Receptor

• Type:

  Reference compound

• Related Pathways:

  GPCR/G Protein

• Applications:

  COVID-19-immunoregulation

• Field of Research:

  Inflammation/Immunology; Endocrinology

• Assay Protocol:

  https://www.medchemexpress.com/oc000459.html

• Purity:

  98.12

• Solubility:

  DMSO : 10 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : < 0.1 mg/mL (ultrasonic)

• Smiles:

  O=C(O)CN1C(C)=C(CC2=NC3=CC=CC=C3C=C2)C4=C1C=CC(F)=C4

• Molecular Formula:

  C21H17FN2O2

• Molecular Weight:

  348.37

• References & Citations:

  [1]Pettipher R, Vinall SL, Xue L, 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. J Pharmacol Exp Ther. 2012 Feb;340 (2) :473-82.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  4°C (Powder, stored under nitrogen)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 2

• Isoform:

  DP

• CAS Number:

  [851723-84-7]