CAS NO: | 161314-17-6 |
包装 | 价格(元) |
5mg | 电议 |
25mg | 电议 |
Physical Appearance | A solid |
Storage | Store at RT |
M.Wt | 316.4 |
Cas No. | 161314-17-6 |
Formula | C13H20N2O5S |
Synonyms | N-Isobutyl-N-(4-methoxyphenylsulfonyl)glycyl Hydroxamic Acid,Matrix Metalloproteinase-3 Inhibitor II,MMP-3 Inhibitor II |
Solubility | ≤25mg/ml in ethanol;100mg/ml in DMSO |
Chemical Name | N-hydroxy-2-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-acetamide |
Canonical SMILES | ONC(CN(S(C1=CC=C(OC)C=C1)(=O)=O)CC(C)C)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Ki: 9, 2.6, 4.3, 3.1, and 17 nM for MMP-8, -9, -12, -13, and -20, respectively.
NNGH is an inhibitor of MMPs.
Matrix metalloproteinases (MMPs), a large class of strictly-related zincdependent enzymes, belong to the family of proteolytic enzymes. MMPs are involved in various aspects of physiological cellular processes and pathologies, such as pulmonary emphysema, reumathoid arthritis, tumor growth and metastasis.
In vitro: Previous study found that NNGH was one of the most prominent representatives of a family of nanomolar inhibitors for some MMPs. In addition, the X-Ray structure of the NNGH-MMP-12 complex showed that the interaction of NNGH with the active site of the enzyme involved the binding of the hydroxamic functional group to the catalytic Zn ion and the binding of the aromatic group to the S1 subsite [1].
In vivo: Previous animal study found that the repeated administration of NNGH to WT mice was able to block the MMP-3 levels, which could reduce the number of adherent retinal leukocytes by 60% as compared to vehicle-treated mice. In addition, the administration of NNGH could even lead to a more pronounced decrease in leukocyte adhesion and the treatment of MMP-3-/- mice with NNGH showed a reduced hypothermic response as compared to vehicle-injected MMP-3-/- mice [2].
Clinical trial: Up to now, NNGH is still in the preclinical development stage.
References:
[1] E. Attolino, V. Calderone, E. Dragoni, et al. Structure-based approach to nanomolar, water soluble matrix metalloproteinases inhibitors (MMPIs). European Journal of Medicinal Chemistry (2010).
[2] Inge Van Hove et al. MMP-3 Deficiency Alleviates Endotoxin-Induced Acute Inflammation in the Posterior Eye SegmentInt J Mol Sci. 2016 Nov; 17(11): 1825.