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Xcess新型高效神经保护分子P7C32014年10月13日03:55 | 新闻印刷版刚刚在上个月的Cell中发表，最近关于神经保护小分子P7C3的 MOA研究具有广泛的体外和体内活性，为研究共享其他常见组织的神经系统疾病，损伤，发育和退行性疾病提供了新的令人兴奋的机会机制。 P7C3 是直接从体内神经发生筛选中鉴定出的无毒，稳定且可口服生物利用的合成小分子。它可以保护齿状回中的新生神经元，并刺激新神经元的生长。它还可以增强老年大鼠的学习和记忆能力。在爆炸介导的创伤性脑损伤（TBI）的啮齿动物模型中，P7C3还可以在损伤后，在神经元细胞死亡发生之前保持轴突的完整性。MOA研究表明P7C3可以结合烟酰胺磷酸核糖基转移酶（NAMPT），这是一种将烟酰胺转化为烟酰胺腺嘌呤二核苷酸（NAD）的限速酶。将活性P7C3化学物质施用至用阿霉素处理的细胞（诱导NAD耗竭），可导致细胞内NAD水平反弹，并免受阿霉素介导的毒性的影响。 如何订购： Xcess Biosciences是一家领先的试剂和服务公司，提供10 mM DMSO溶液和以克计的固体形式的化合物。请访问我们的网站以获取订单信息和其他创新产品。特别是Xcess Biosciences继续向我们的表观遗传调节剂工具箱 （现在我们提供72种独特的化合物）和 泛素调节剂工具箱 （现在我们提供15种独特的化合物）中添加了更多新颖的小分子化学探针 。
Product Information
| Molecular Weight: | 518.36 |
| Formula: | C25H20BrN5O3 |
| Purity: | >98% |
| CAS#: | 916170-19-9 |
| Solubility: | DMSO: ≥ 51 mg/mL |
| Chemical Name: | (E)-N-(2-(2-(1-(3-bromophenyl)ethylidene)hydrazinyl)-2-oxo-1-(4-oxo-3,4-dihydrophthalazin-1-yl)ethyl)benzamide |
| Storage: | Powder -20oC 3 years 4oC 2 yearsIn solvent -80oC 6 months-20oC 1 month |
Biological Activity:
AC-55541 is a novel small-molecule protease-activated receptor 2(PAR2) agonist; activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assays, with potencies ranging from 200 to 1000 nM. IC50 value: 200-1000 nM(EC50) [1] Target: PAR2 agonist Neither AC-55541 nor AC-264613 had activity at any of the other PAR receptor subtypes, nor did they have any significant affinity for over 30 other molecular targets involved in nociception. Visualization of EYFP-tagged PAR2 receptors showed that each compound stimulated internalization of PAR2 receptors. AC-55541 was well absorbed when administered intraperitoneally to rats, reaching micromolar peak plasma concentrations. AC-55541 was stable to metabolism by liver microsomes and maintained sustained exposure in rats, with elimination half-lives of 6.1 h. Intrapaw administration of AC-55541 or AC-264613 elicited robust and persistent thermal hyperalgesia and edema. Coadministration of either a tachykinin 1 (neurokinin 1) receptor antagonist or a transient receptor potential vanilloid (TRPV) 1 antagonist completely blocked these effects. Systemic administration of either AC-55541 or AC-264613 produced a similar degree of hyperalgesia as was observed when the compounds were administered locally.
Reference:
[1]. Gardell LR, et al. Identification and characterization of novel small-molecule protease-activated receptor 2 agonists. J Pharmacol Exp Ther. 2008 Dec;327(3):799-808.
