ML380 is a highly potent and the first CNS penetrant M5 positive allosteric modulator (PAM).
仅供研究使用。 我们不向患者出售。
名称 | ML380 |
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Iupac 化学名称 | 1-((1H-indazol-5-yl)sulfonyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide |
同义词 | ML380 ; ML 380 ; ML-380 |
英文同义词 | ML380 ; ML 380 ; ML-380 |
分子式 | C23H25F3N4O3S |
分子量 | 494.53 |
Smile | CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F |
InChiKey | FJPQEOQGIZSLES-UHFFFAOYSA-N |
InChi | InChI=1S/C23H25F3N4O3S/c1-2-29(15-17-5-3-4-6-20(17)23(24,25)26)22(31)16-9-11-30(12-10-16)34(32,33)19-7-8-21-18(13-19)14-27-28-21/h3-8,13-14,16H,2,9-12,15H2,1H3,(H,27,28) |
Cas号 | 1627138-52-6 |
相关CAS号 | 1627138-52-6 |
包装 | 价格 | 库存 | 纯度 | 备货期 |
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大货 | 询价 | 询价 | 询价 |
外观性状 | 类白色至白色固体 |
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纯度 | ≧98.0% |
存储 | 短期(几天到几周)为0-4摄氏度,长期(几个月)为-20摄氏度 |
可溶性 | 可溶于DMSO |
处理方式 | Avoid inhalation, contact with eyes and skin. Avoid dust and aerosol formation. Use only in areas with appropriate exhaust ventilation. |
运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周 |
海关编码 | 2933999701 |
Targets | |
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Mechanism | |
Cell study | |
Animal study | |
Clinical study |
1: Berizzi AE, Gentry PR, Rueda P, Den Hoedt S, Sexton PM, Langmead CJ, Christopoulos A. Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators. Mol Pharmacol. 2016 Oct;90(4):427-36. doi: 10.1124/mol.116.104182. PubMed PMID: 27461343.
2: Gentry PR, Kokubo M, Bridges TM, Daniels JS, Niswender CM, Smith E, Chase P, Hodder PS, Rosen H, Conn PJ, Engers J, Brewer KA, Lindsley CW, Wood MR. Development of the First CNS penetrant M5 Positive Allosteric Modulator (PAM) Based on a Novel, non-Isatin Core. 2013 Dec 15 [updated 2015 Feb 11]. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. Available from http://www.ncbi.nlm.nih.gov/books/NBK280054/ PubMed PMID: 25834908.
3: Gentry PR, Kokubo M, Bridges TM, Noetzel MJ, Cho HP, Lamsal A, Smith E, Chase P, Hodder PS, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR. Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4- carboxamide (ML380). J Med Chem. 2014 Sep 25;57(18):7804-10. doi: 10.1021/jm500995y. PubMed PMID: 25147929; PubMed Central PMCID: PMC4175000.