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蚂蚁淘在线 / 品牌中心 / Xcess / Xcessbio/SAG, Hedgehog Agonist-Xcessbio Biosciences Inc/10 mM DMSO (0.408 mL)/M60081-2
商品描述
Details
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: | 490.06 |
| Formula: | C28H28ClN3OS |
| Purity: | ≥ 98% |
| CAS#: | 364590-63-6 |
| Solubility: | DMSO up to 50 mM |
| Chemical Name: | 3-chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide |
| Storage: | Powder:4oC 1 year. DMSO:4oC3 month;-20oC 1 year. |
Biological Activity:
SAG is a potent, selective, and cell-permeable small-molecule agonist of the Hedgehog pathway. It modulates the coupling of Smo with its downstream effector by interacting with the Smo heptahelical domain (KD = 59 nM). SAG induces Hedgehog pathway activation with an EC50 of ~3 nM in NIH 3T3-derived Shh-LIGHT2 cells and counteracts Cyclopamine-KAAD inhibition of Smo. It was reported that SAG acts as an activator at low concentrations and as an inhibitor at high concentrations (>1 µM). In recent studies, SAG was shown to prevent glucocorticoid-induced neonatal cerebellar injury, and trigger rapid metabolic rewiring via AMPK.
How to Use:
- In vitro: SAG was used at 200 nM to induce Hh pathway activation.
- In vivo: n/a
Reference:
- 1. Frank-Kamenetsky M, et al. Small-molecule modulators of Hedgehog signaling: identification and characterization of Smoothened agonists and antagonists. (2002) Journal of Biology (1): 10.2-10.19.
- 2. Chen JK, et al. Small molecule modulation of Smoothened activity.(2002) Proc Natl Acad Sci U S A. 99(22):14071-6.
- 3. Chen W, et al. Activity-dependent internalization of smoothened mediated by beta-arrestin 2 and GRK2. (2004) Science. 306(5705):2257-60.
- 4. Dyer LA, et al. BMP signaling modulates hedgehog-induced secondary heart field proliferation. (2010) Dev Biol. 348(2):167-76.
- 5. Heine VM, et al. A small-molecule smoothened agonist prevents glucocorticoid-induced neonatal cerebellar injury. (2011) Sci Transl Med. 3(105).
- 6. Teperino R, et al. Hedgehog partial agonism drives Warburg-like metabolism in muscle and brown fat. (2012) Cell. 151(2):414-26.
SAG_spec.pdf- SAG_MSDS.pdf
Products are for research use only. Not for human use.
