AZD1981
更新时间：2024-07-15 12:36:53
采购访问：17次
| 常用名 | 4-(乙酰氨基)-3-[(4-氯苯基)硫代]-2-甲基-1H-吲哚-1-乙酸 | CAS号 | 802904-66-1 |
|---|---|---|---|
| 价格 | 纯度 | 98.0% | |
| 备货期 | 10天 | 库存 | 现货 |
| 产品详情（用途，包装等）
用途： AZD1981 is a potent and selective CRTh2 antagonist; displaces radio-labelled PGD2 from human recombinant DP2 with high potency (pIC50 = 8.4).IC50 value:Target: GPR44 antagonistin vitro: AZD1981 produced a concentration-dependent displacement of the [3H]PGD2-specific binding with a mean pIC50 of 8.4 ± 0.1 (n = 25, geometric mean IC50 of 4 nM). AZD1981 had no significant affinity towards recombinant human DP1 receptors with only a mean 27% (range 14–50%; n = 4) displacement of [3H]PGD2-specific binding observed at the highest concentration tested (10 μM). Compared with the binding potency for DP2, AZD1981 showed 10-fold selectivity over rat aldose reductase and 1700-fold selectivity over rat steroid 5α-reductase.In eosinophils, a single concentration of 1 μM, AZD1981 caused a large (20-fold) rightward parallel shift in the 15R-methyl PGD2 E/[A] curve with no evidence of a decrease in the maximal response. The effect of AZD1981 was therefore investigated using a single sub-maximal concentration of agonist (1 μM). AZD1981 produced a concentration-dependent inhibition of eosinophil migration with a pIC50 value of 7.6 ± 0.1 (n = 4) [1].in vivo: Using the previously described guinea pig hind limb model , 10 nM AZD1981 significantly inhibited DK-PGD2-induced eosinophil mobilization by approximately 50%, and the response was completely inhibited with 100 nM AZD1981 [1]. in vivo: AZD1981 exhibited good cross-species binding activity against mouse, rat, guinea pig, rabbit and dog DP2 . Evaluation in mouse, rat or rabbit cell systems was not possible as they did not respond to DP2 agonists. Agonist responses were seen in guinea pig and dog, and AZD1981 blocked DP2 -mediated eosinophil shape change. Such responses were more robust in the guinea pig, where AZD1981 also blocked DP2 -dependent eosinophil emigration from bone marrow [1]. There was no beneficial clinical effect of AZD1981, at a dose of 1000 mg twice daily for 4 weeks, in patients with moderate to severe COPD. AZD1981 was well tolerated and no safety concerns were identified [3]. 物理化学性质： CAS号：802904-66-1 常用中文名：4-(乙酰氨基)-3-[(4-氯苯基)硫代]-2-甲基-1H-吲哚-1-乙酸 常用英文名：AZD1981 分子式：C19H17ClN2O3S 分子量：388.86800 密度：N/A 沸点：N/A 熔点：N/A 闪点：N/A 储存条件：-20°C |
上海念兴实业有限公司
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- 上海阿拉丁生化科技股份有限公司
- 上海市 上海市 浦东新区
- 产品名：AZD1981
- 价格： ￥1968.9/25mg ￥535.9/5mg ￥需询单/1g ￥需询单/1g
- 纯度：98.0%
- 备货期：1天
- 联系人：阿拉丁
- 上海化源世纪贸易有限公司
- 上海市 上海市 普陀区
- 产品名：AZD1981
- 价格：
- 纯度：98.0%
- 备货期：10天
- 联系人：徐经理
- 上海阿摩尔生物科技有限公司
- 上海市 上海市 奉贤区
- 产品名：AZD1981游离态
- 价格： ￥需询单/100mg ￥需询单/10mg ￥需询单/1g ￥需询单/1mg
- 纯度：99.0%
- 备货期：需询单
- 联系人：王汐瑶
- 武汉敬康恩生物医药科技有限公司
- 湖北省 武汉市 东西湖区
- 产品名：AZD1981
- 价格： ￥需询单/1g ￥需询单/5g
- 纯度：98.0%
- 备货期：需询单
- 联系人：周经理
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4-(乙酰氨基)-3-[(4-氯苯基)硫代]-2-甲基-1H-吲哚-1-乙酸生产厂家
参考价格：$86/10mM*1mLinDMSO