NNGH
(Synonyms: N-Isobutyl-N-(4-methoxyphenylsulfonyl)glycyl Hydroxamic Acid,Matrix Metalloproteinase-3 Inhibitor II,MMP-3 Inhibitor II) 目录号 : GC15726A broad-spectrum MMP inhibitor
Cas No.:161314-17-6
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: ≥99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
Cas No. | 161314-17-6 | SDF | |
别名 | N-Isobutyl-N-(4-methoxyphenylsulfonyl)glycyl Hydroxamic Acid,Matrix Metalloproteinase-3 Inhibitor II,MMP-3 Inhibitor II | ||
化学名 | 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 | ||
分子式 | C13H20N2O5S | 分子量 | 316.4 |
溶解度 | ≤25mg/ml in ethanol;100mg/ml in DMSO | 储存条件 | RT |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.1606 mL | 15.8028 mL | 31.6056 mL |
5 mM | 0.6321 mL | 3.1606 mL | 6.3211 mL |
10 mM | 0.3161 mL | 1.5803 mL | 3.1606 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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