MCUF-651 is a small molecule guanylyl cyclase A receptor positive allosteric modulator (GC-A PAM). MCUF-651 enhanced ANP-mediated cGMP generation in human cardiac, renal, and fat cells and inhibited cardiomyocyte hypertrophy in vitro. Further, binding analysis confirmed MCUF-651 binds to GC-A and selectively enhances the binding of ANP to GC-A. Moreover, MCUF-651 is orally bioavailable in mice and enhances the ability of endogenous ANP and BNP, found in the plasma of normal subjects and patients with hypertension or heart failure, to generate GC-A-mediated cGMP ex vivo.
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名称 | MCUF-651 |
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Iupac 化学名称 | N-(4,6-difluorobenzo[d]thiazol-2-yl)-1-(2-(dimethylamino)ethyl)piperidine-3-carboxamide |
同义词 | MCUF-651; MCUF 651 MCUF651; |
英文同义词 | MCUF-651; MCUF 651 MCUF651; |
分子式 | C17H22F2N4OS |
分子量 | 368.44 |
Smile | O=C(C1CN(CCN(C)C)CCC1)NC2=NC3=C(F)C=C(F)C=C3S2 |
InChiKey | NOPAIELWJAFUCL-UHFFFAOYSA-N |
InChi | InChI=1S/C17H22F2N4OS/c1-22(2)6-7-23-5-3-4-11(10-23)16(24)21-17-20-15-13(19)8-12(18)9-14(15)25-17/h8-9,11H,3-7,10H2,1-2H3,(H,20,21,24) |
Cas号 | 2747162-85-0 |
相关CAS号 |
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 | 固体粉末 |
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纯度 | 98% Min. |
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 | 溶于DMSO |
处理方式 | |
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. |
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Mechanism | |
Cell study | |
Animal study | |
Clinical study |
1: Sangaralingham SJ, Kuhn M, Cannone V, Chen HH, Burnett JC. Natriuretic peptide pathways in heart failure: further therapeutic possibilities. Cardiovasc Res. 2023 Feb 3;118(18):3416-3433. doi: 10.1093/cvr/cvac125. PMID: 36004816; PMCID: PMC9897690.
2: Sangaralingham SJ, Whig K, Peddibhotla S, Kirby RJ, Sessions HE, Maloney PR, Hershberger PM, Mose-Yates H, Hood BL, Vasile S, Pan S, Zheng Y, Malany S, Burnett JC Jr. Discovery of small molecule guanylyl cyclase A receptor positive allosteric modulators. Proc Natl Acad Sci U S A. 2021 Dec 28;118(52):e2109386118. doi: 10.1073/pnas.2109386118. PMID: 34930837; PMCID: PMC8719854.