Timapiprant (OC000459) is a potent, selective, and orally active D prostanoid receptor 2 (DP₂, also known asCRTH2) antagonist. Timapiprant (OC000459) potently displaces [³H] PGD2 from human recombinantDP₂(K_i=13 nM), rat recombinantDP₂(K_i=3 nM), and human nativeDP₂(K_i=4 nM). Timapiprant (OC000459) 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 (OC000459) (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 (OC000459) (1 μM) inhibits the activation of Th2 cells and eosinophils in response to supernatants from IgE/anti-IgE-activated human mast cells^[1].
Timapiprant (OC000459) (1 nM–1000 nM; 16 hours) inhibits the anti-apoptotic effect of PGD2 on Th2 cells with an IC₅₀of 0.035 uM^[1].

Timapiprant (OC000459) (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 (OC000459) (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].

348.37

Solid

C₂₁H₁₇FN₂O₂

851723-84-7

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)

DMSO : 10 mg/mL(28.71 mM;ultrasonic and warming and heat to 60℃)

H₂O :< 0.1 mg/mL(insoluble)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 0.4 mg/mL (1.15 mM); Clear solution

  此方案可获得 ≥ 0.4 mg/mL (1.15 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 4.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液