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Timapiprant {[allProObj[0].p_purity_real_show]}

货号:A894984 同义名: OC000459

OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM.

Timapiprant 化学结构 CAS号:851723-84-7
Timapiprant 化学结构
CAS号:851723-84-7
Timapiprant 3D分子结构
CAS号:851723-84-7
Timapiprant 化学结构 CAS号:851723-84-7
Timapiprant 3D分子结构 CAS号:851723-84-7
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Timapiprant 纯度/质量文件 产品仅供科研

货号:A894984 标准纯度: {[allProObj[0].p_purity_real_show]}
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Timapiprant 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].

Timapiprant 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 <<

Timapiprant 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.

Timapiprant 实验方案

计算器
存储液制备 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

Timapiprant 技术信息

CAS号851723-84-7
分子式C21H17FN2O2
分子量 348.37
SMILES Code CC1=C(CC2=NC3=C(C=CC=C3)C=C2)C2=C(C=CC(F)=C2)N1CC(O)=O
MDL No. MFCD18633254
别名 OC000459
运输蓝冰
InChI Key FATGTHLOZSXOBC-UHFFFAOYSA-N
Pubchem ID 11462174
存储条件

In solvent -20°C:3-6个月-80°C:12个月

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

溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案一
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