Timapiprant

产品说明书

Print
Chemical Structure| 851723-84-7 同义名 : OC000459
CAS号 : 851723-84-7
货号 : A894984
分子式 : C21H17FN2O2
纯度 : 98%
分子量 : 348.37
MDL号 : MFCD18633254
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • GPR

    DP2, IC50:13 nM

  • GPR

    DP2, IC50:13 nM
描述 D prostanoid receptor 2 (DP2) is selectively expressed by T helper 2 (Th2) lymphocytes, eosinophils, and basophils and mediates recruitment and activation of these cell types in response to prostaglandin D2 (PGD2)[1]. OC000459 is a potent, selective, and orally active DP2 antagonist. It potently displaces [3H] PGD2 from human recombinant DP2 (Ki = 13 nM), rat recombinant DP2 (Ki = 3 nM), and human native DP2 (Ki = 4 nM). OC000459 inhibited chemotaxis (IC50 = 0.028 μM) of human Th2 lymphocytes and cytokine production (IC50 = 0.019 μM) by human Th2 lymphocytes. OC000459 also inhibited the activation of Th2 cells and eosinophils in response to supernatants from IgE/anti-IgE-activated human mast cells[1]. OC000459 was found to be orally bioavailable in rats and effective in inhibiting blood eosinophilia induced by 13, 14-dihydro-15-keto-PGD2 (DK-PGD2) in this species (ED50 = 0.04 mg/kg p.o.) and airway eosinophilia in response to an aerosol of DK-PGD2 in guinea pigs (ED50 = 0.01 mg/kg p.o.)[1].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00290381 Allergic Rhinitis Phase 1 Completed - United Kingdom ... 展开 >> National Heart & Lung Institute Clinical Studies Unit London, United Kingdom, SW3 6HP 收起 <<
NCT02660489 Asthma Rhinov... 展开 >>irus Picornaviridae Infections Common Cold 收起 << Phase 2 Unknown February 2018 United Kingdom ... 展开 >> St Mary's Hospital Recruiting London, Greater London, United Kingdom, W2 1PG Contact: Hugo Farne, BMBCh MA    07590 250487    asthma.trial@imperial.ac.uk    Contact: Maria-Belén Trujillo-Torralbo, BSc    07590 250487    asthma.trial@imperial.ac.uk 收起 <<
NCT00697281 Allergic Rhinitis Phase 2 Completed - Austria ... 展开 >> Allergie Zentrum Wien West, Vienna Challenge Chamber Vienna, Austria, 1150 VIENNA 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.87mL

0.57mL

0.29mL

14.35mL

2.87mL

1.44mL

28.71mL

5.74mL

2.87mL
参考文献

[1]Pettipher R, Vinall SL, Xue L, et al. 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;340(2):473–482.

[2]Pettipher R, Vinall SL, et al. 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.

[3]340(2):473–482.