| CAS NO: | 544678-85-5 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 410.4 |
| Cas No. | 544678-85-5 |
| Formula | C22H20F2N4O2 |
| Synonyms | Collagenase-3 Inhibitor,Matrix Metalloproteinase-13 Inhibitor,4,6-Pyrimidinedicarboxamide |
| Solubility | ≤0.5mg/ml in ethanol;2mg/ml in DMSO;2mg/ml in dimethyl formamide |
| Chemical Name | N4,N6-bis[(4-fluoro-3-methylphenyl)methyl]-4,6-pyrimidinedicarboxamide |
| Canonical SMILES | FC1=C(C)C=C(CNC(C2=CC(C(NCC3=CC=C(F)C(C)=C3)=O)=NC=N2)=O)C=C1 |
| 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。 |
IC50: 8 nM
MMP-13 Inhibitor is a MMP-13 inhibitor.
Matrix metalloproteinases (MMPs), a family of zinc endopeptidases, can degrade proteins of the extracellular matrix, such as collagens, elastins, matrix glycoproteins, and proteoclycans. Zymogen activation and endogenous tissue inhibitors of matrix metalloproteinases control MMP activity during normal morphogenesis and tissue homeostasis. Abnormal expression or activity of MMPs has been reported to be related with pathological processes including metastasis, angiogenesis, cardiovascular disease, and rheumathoid arthritis and osteoarthritis.
In vitro: MMP-13 Inhibitor was previously synthesized as a pyrimidine dicarboxamide that could inhibit the matrix metalloproteinase-13 (MMP-13) with the IC50 of 8 nM. Moreover, MMP-13 Inhibitor was found to be able to bind to MMP pockets that are unique to MMP-13 rather than the catalytic zinc, and therefore was specific for MMP-13 over other MMPs. In addition, during endochondral ossification, MMP-13 Inhibitor could also block osterix-dependent calcification of matrices in limb bud cells [1, 2, 3].
In vivo: So far, there is no animal in vivo study reported.
Clinical trial: So far, no clinical study has been conducted.
References:
1. Carrascal, N.A. and Rizzo, R.C. Calculation of binding free energies for non-zinc chelating pyrimidine dicarboxamide inhibitors with MMP-13. Bioorg.Med.Chem.Lett. 19(1), (2009).
2. Engel, C.K.,Pirard, B.,Schimanski, S., et al. Structural basis for the highly selective inhibition of MMP-13. Chem.Biol. 12(2), 181-189 (2005).
3. Nishimura, R.,Wakabayashi, M.,Hata, K., et al. Osterix regulates calcification and degradation of chondrogenic matrices through matrix metalloproteinase 13 (MMP13) expression in association with transcription factor Runx2 during endochondral ossification. J.Biol.Chem. 287(40), 33179-33190 (2012).
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