OC000459

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更新时间： 2025-08-24 17:59:29

CAS号：851723-84-7

常用名： Timapiprant

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纯度： 98.0%

备货期： 10天

库存： 现货

其他详情（用途，包装）：
用途： OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM.IC50 Value: 13 nM( Ki for hrCRTH2); 3 nM( Ki for Rat rCRTH2);13 nM(Ki for human native CRTH2)Target: D prostanoid receptor 2CRTH2 (chemoattractant receptor expressed on T-helper (Th) type 2 cells) is a G-protein-coupled receptor expressed by Th2 lymphocytes and eosinophils that mediates prostaglandin (PG)D(2)-driven chemotaxis[1]. CRTH2 mediates activation of Th2 cells, eosinophils and basophils in response to prostaglandin D(2). The CRTH2 antagonist OC000459 has been demonstrated to reduce airway inflammation and improve lung function in moderate persistent asthma[2].in vitro: OC000459 is an indole-acetic acid derivative that potently displaces [3H]PGD2from human recombinant DP2 (Ki = 0.013 μM), rat recombinant DP2 (Ki = 0.003 μM), and human native DP2 (Th2 cell membranes; Ki = 0.004 μM) but does not interfere with the ligand binding properties or functional activities of other prostanoid receptors (prostaglandin E1-4 receptors, D prostanoid receptor 1, thromboxane receptor, prostacyclin receptor, and prostaglandin F receptor). OC000459 inhibited chemotaxis (IC50 = 0.028 μM) of human Th2 lymphocytes and cytokine production (IC50 = 0.019 μM) by human Th2 lymphocytes. OC000459 competitively antagonized eosinophil shape change responses induced by PGD2 in both isolated human leukocytes (pKB = 7.9) and human whole blood (pKB = 7.5) but did not inhibit responses to eotaxin, 5-oxo-eicosatetraenoic acid, or complement component C5a. OC000459 also inhibited the activation of Th2 cells and eosinophils in response to supernatants from IgE/anti-IgE-activated human mast cells. OC000459 had no significant inhibitory activity on a battery of 69 receptors and 19 enzymes including cyclooxygenase 1 (COX1) and COX2[3] .in vivo: 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.) [3].Clinical trial: N/A. 物理化学性质： CAS号：851723-84-7 常用中文名：Timapiprant 常用英文名：OC000459 分子式：C21H17FN2O2 分子量：348.370 密度：1.3±0.1 g/cm3 沸点：574.4±50.0 °C at 760 mmHg 熔点：N/A 闪点：301.2±30.1 °C 储存条件：-20°C

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公司名：上海化源世纪贸易有限公司推荐

认证状态： 已认证供应商

商品数： 396716件

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公司介绍：
化源网，2015 年正式成立，是专注服务全球精细化学与生物医药研发领域的专业社群电商平台。
平台严选优质品牌商家直供，以正品低价为核心优势，搭配简洁易操作的商城界面，为研发人员提供一站式采购方案，全程保障高效便捷的服务体验。

其他供应商价格：

2022-02-19 价格：￥662.9 OC000459

2021-02-06 价格：￥603.0 OC000459

2017-08-07 价格：￥需询单 OC000459

2024-05-23 价格：￥需询单 OC000459

2023-09-13 价格：￥需询单 OC000459

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Timapiprant价格

OC000459

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