950688-14-9

950688-14-9 structure

Name: Timapiprant sodium
Chemical Name: Timapiprant sodium
CAS Number: 950688-14-9
Molecular Formula: C₂₁H₁₇FN₂NaO₂+
Molecular Weight: 371.36
Catalog: Signaling Pathways GPCR/G Protein Prostaglandin Receptor
Create Date: 2019-08-04 11:16:59
Modify Date: 2024-01-09 16:47:13
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].

Name	Timapiprant sodium

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].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor Research Areas >> Inflammation/Immunology
Target	Ki: 0.013 μM (human recombinant DP2); 0.003 μM (rat recombinant DP2) and 0.004 μM (human native DP2)[1]
In Vitro	Timapiprant sodium (OC000459 sodium) (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[1]. Timapiprant sodium (OC000459 sodium) (1 μM) inhibits the activation of Th2 cells and eosinophils in response to supernatants from IgE/anti-IgE-activated human mast cells[1]. Timapiprant sodium (OC000459 sodium) (1 nM–1000 nM; 16 hours) inhibits the anti-apoptotic effect of PGD2 on Th2 cells with an IC50 of 0.035 uM[1]. Apoptosis Analysis[1] Cell Line: Th2 Cells Concentration: 0.0001 μM-10 μM Incubation Time: 16 hours Result: Inhibited the antiapoptotic effect of PGD2.
In Vivo	Timapiprant sodium (OC000459 sodium) (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)[1]. Timapiprant sodium (OC000459 sodium) (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)[1].
References	[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.

Molecular Formula	C₂₁H₁₇FN₂NaO₂+
Molecular Weight	371.36

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