| 品牌 | 货号 | 产品规格 | 价格(RMB) | 库存（上海） | 北京 | 武汉 | 南京 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
| 源叶(MedMol) | S81448-5mg | ≥98%(HPLC) | ￥280.00元 | 5 | - | - | - |
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| 源叶(MedMol) | S81448-10mg | ≥98%(HPLC) | ￥520.00元 | 5 | - | - | - |
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| 源叶(MedMol) | S81448-50mg | ≥98%(HPLC) | ￥2590.00元 | 5 | - | - | - |
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| 源叶(MedMol) | S81448-100mg | ≥98%(HPLC) | ￥5150.00元 | 6 | - | - | - |
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| 产品描述： ESI-09 is a novel noncyclic nucleotide EPAC antagonist with IC50 values of 3.2 and 1.4 μM for EPAC1 and EPAC2, respectively. | ||||||||||||||||||||
| 靶点： IC50: 3.2 μM (EPAC1), 1.4 μM (EPAC2);cAMP; VirusProtease | ||||||||||||||||||||
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体外研究： While cAMP competes with 8-NBD-cAMP binding with an IC50 of 39 µM, ESI-09 shows an increased potency with an apparent IC50 of 10 µM. ESI-09 inhibis cAMP-mediated EPAC2 and EPAC1 GEF activity with an IC50 of 1.4 and 3.2µM, respectively. ESI-09 could fit well into the functional cAMP-binding pocket of EPAC1, establishing favorable hydrophobic and hydrogen bonding interactions with the protein’s active-site residues. ESI-09 inhibits 007-AM-stimulated Akt phosphorylation at T308 and S473 in a dose-dependent manner. ESI-09 inhibits pancreatic cancer cells AsPC-1 and PANC-1 migration. ESI-09 inhibits EPAC1-mediated adhesion of PDA cells on collagen I. Exposure to ESI-09 significantly reduces intracellular and total bacterial counts in HUVECs at 30 min postinfection with 10 multiplicities of infection (MOI) of R. australis compared with similarly infected controls |
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体内研究： Treatment with ESI-09 dramatically protects WT mice against R. australis infection with much milder disease manifestations and significantly improves survival |
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参考文献： 1. Almahariq M, et al. A novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasion. Mol Pharmacol. 2013 Jan;83(1):122-8. 2. Gong B, et al. Exchange protein directly activated by cAMP plays a critical role in bacterial invasion during fatal rickettsioses. Proc Natl Acad Sci U S A. 2013 Nov 26;110(48):19615-20. |
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| 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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