Timapiprant sodium (OC000459 sodium) 是一种高效选择性的口服型 D 前列腺素受体 2 (DP₂，也称为 CRTH2) 拮抗剂。Timapiprant sodium (OC000459 sodium) 有效地置换来自人重组 DP₂ (K _i=13 nM)，大鼠重组 DP₂ ( K _i=3 nM) 和人天然 DP₂ ( K _i=4 nM) 的 [³H] PGD2。 Timapiprant sodium (OC000459 sodium) 抑制肥大细胞激活 Th2 淋巴细胞和嗜酸性粒细胞。

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

Solid

Ki: 0.013 μM (human recombinant DP2); 0.003 μM (rat recombinant DP2) and 0.004 μM (human native DP2)

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.
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.
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.
has not independently confirmed the accuracy of these methods. They are for reference only.

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 (ED 50 =0.04 mg/kg).
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 (ED 50 =0.01 mg/kg).
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

[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.

In Vitro: DMSO : 100 mg/mL (270.01 mM; Need ultrasonic)配制储备液