產(chǎn)品屬性：

Cas No.: 950688-14-9

別名: N/A

化學(xué)名: N/A

分子式: C21H17FN2NaO2+

分子量: 371.36

溶解度: DMSO: 100 mg/mL (270.01 mM)

儲(chǔ)存條件: Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.

Shipping ConditionEvaluation sample solution : ship with blue ice

All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

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].Ki: 0.013 μM (human recombinant DP2); 0.003 μM (rat recombinant DP2) and 0.004 μM (human native DP2)[1]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 CellsTimapiprant 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].[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.
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