| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
T73707-5mg促销 |
≥95% | ￥1080.00 ￥975.00 |
8 | 3 | 2 | - | - |
|
T73707-25mg促销 |
≥95% | ￥3810.00 ￥3420.00 |
4 | 3 | 2 | - | - |
|
| 产品描述： | CID 2745687 acts as a specific, reversible and competitive GPR35 antagonist with a Ki of 12.8 nM | ||||||||||||||||||||
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| 靶点： | GPR35;GPR | ||||||||||||||||||||
| 体外研究： | For ERK1/2 phosphorylation with 1 μM Pamoic acid as the agonist, the CID 2745687 (CID2745687) Ki is 18 nM. CID 2745687 (CID-2745687) is a potent antagonist in β-arrestin-2 interaction assays only at human GPR35.Using the BRET-based GPR35-β-arrestin-2 interaction assay and an EC80 concentration of Zaprinast (20 μM) as agonist, CID 2745687 behaved as a moderately potent, concentration-dependent antagonist at human GPR35 with pIC50=6.70±0.09. CID 2745687 (pIC50=6.27±0.08) fully reverses the agonist action of Cromolyn disodium | ||||||||||||||||||||
| 体内研究： | CID 2745687 (CID2745687; 1 mg/kg; administrated orally every day for the last 4 weeks), a specific GPR35 antagonist, reverses Lodoxamide-mediated anti-fibrotic effects. Animal Model: Six-week-old male C57BL/6 mice Dosage: 1 mg/kg Administration: Oral administration, every day for 4 weeks Result: Inhibited Lodoxamide-mediated protective effects. | ||||||||||||||||||||
| 参考文献： | 1. Pingwei Zhao, et al. Targeting of the orphan receptor GPR35 by pamoic acid: a potent activator of extracellular signal-regulated kinase and β-arrestin2 with antinociceptive activity. Mol Pharmacol. 2010 Oct;78(4):560-8. 2. Laura Jenkins, et al. Antagonists of GPR35 display high species ortholog selectivity and varying modes of action. J Pharmacol Exp Ther. 2012 Dec;343(3):683-95. 3. Mi-Jeong Kim, et al. Lodoxamide Attenuates Hepatic Fibrosis in Mice: Involvement of GPR35. Biomol Ther (Seoul). 2019 Jun 13;28(1):92-97. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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