中文名 | SAG hydrochloride |
英文名 | SAG hydrochloride |
别名 | SAG盐酸盐 REL-3-氯-N-((1R,4R)-4-(甲基氨基)环己基)-N-(3-(吡啶-4-基)苄基)苯并[B]噻吩-2-甲酰胺盐酸盐 |
英文别名 | SAG.2HCl SAG hydrochloride rel-3-Chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide hydrochloride |
CAS | 2095432-58-7 |
化学式 | C28H29Cl2N3OS |
分子量 | 526.52 |
溶解度 | 溶于DMSO |
存储条件 | -20℃ |
体外研究 | SAG通过直接结合到Smo螺旋束调控Smo活性。 SAG以GRK2依赖的方式诱导通过Gli的Smo-依赖性信号。 SAG(1 nM)也会诱导神经元和神经胶质前体细胞的增殖,而不影响新生细胞的分化模式。 |
体内研究 | 在成年大鼠海马中,SAG (2.5 nM)脑室内给药显著增加新生细胞的数量,并延长海马细胞的存活时间。在小鼠中,SAG (20 μg/g, i.p.)有效防止GC-诱导的新生小脑发育异常。 |
参考资料 展开查看 | 1: Geyer N, Ridzewski R, Bauer J, Kuzyakova M, Dittmann K, Dullin C, Rosenberger A, Schildhaus HU, Uhmann A, Fulda S, Hahn H. Different Response of Ptch Mutant and Ptch Wildtype Rhabdomyosarcoma Toward SMO and PI3K Inhibitors. Front Oncol. 2018 Sep 25;8:396. doi: 10.3389/fonc.2018.00396. eCollection 2018. PubMed PMID: 30319965; PubMed Central PMCID: PMC6168716. 2: Guerrini G, Criscuoli M, Filippi I, Naldini A, Carraro F. Inhibition of smoothened in breast cancer cells reduces CAXII expression and cell migration. J Cell Physiol. 2018 Dec;233(12):9799-9811. doi: 10.1002/jcp.26947. Epub 2018 Aug 21. PubMed PMID: 30132883. 3: Gigante ED, Long AB, Ben-Ami J, Caspary T. Hypomorphic Smo mutant with inefficient ciliary enrichment disrupts the highest level of vertebrate Hedgehog response. Dev Biol. 2018 May 15;437(2):152-162. doi: 10.1016/j.ydbio.2018.03.019. Epub 2018 Mar 20. PubMed PMID: 29571613; PubMed Central PMCID: PMC5903954. 4: Zhang F, Hao M, Jin H, Yao Z, Lian N, Wu L, Shao J, Chen A, Zheng S. Canonical hedgehog signalling regulates hepatic stellate cell-mediated angiogenesis in liver fibrosis. Br J Pharmacol. 2017 Mar;174(5):409-423. doi: 10.1111/bph.13701. Epub 2017 Jan 31. PubMed PMID: 28052321; PubMed Central PMCID: PMC5301045. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.899 ml | 9.496 ml | 18.993 ml |
5 mM | 0.38 ml | 1.899 ml | 3.799 ml |
10 mM | 0.19 ml | 0.95 ml | 1.899 ml |
5 mM | 0.038 ml | 0.19 ml | 0.38 ml |
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