Timapiprant (sodium)

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].

Product Specifications

CAS Number

[950688-14-9]

Product Name Alternative

OC000459 (sodium)

UNSPSC

12352005

Target

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

Purity

99.61

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 Formula

C21H16FN2NaO2

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.