Timapiprant (sodium)

• UNSPSC Description:

  Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant sodium (OC000459 sodium) 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 sodium (OC000459 sodium) inhibits mast cell activation of Th2 lymphocytes and eosinophils[1].

• Target Antigen:

  Prostaglandin Receptor

• Type:

  Reference compound

• Related Pathways:

  GPCR/G Protein

• Applications:

  Neuroscience-Neuromodulation

• Field of Research:

  Inflammation/Immunology; Endocrinology

• Assay Protocol:

  https://www.medchemexpress.com/timapiprant-sodium.html

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• Smiles:

  O=C(O[Na])CN1C2=CC=C(F)C=C2C(CC3=NC4=C(C=CC=C4)C=C3)=C1C

• Molecular Weight:

  370.35

• References & Citations:

  [1]Singh D, Cadden P, Hunter M, Inhibition of the asthmatic allergen challenge response by the CRTH2 antagonist OC000459. Eur Respir J. 2013 Jan;41(1):46-52.|[2]Horak F, Zieglmayer P, Zieglmayer R, The CRTH2 antagonist OC000459 reduces nasal and ocular symptoms in allergic subjects exposed to grass pollen, a randomised, placebo-controlled, double-blind trial. Allergy. 2012 Dec;67(12):1572-9.|[3]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

• Clinical Information:

  Phase 2

• CAS Number:

  950688-14-9