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Submit ReviewBI 4394 is a highly potent and selective MMP-13 inhibitor (IC50 = 1 nM). BI 4394 inhibits the degradation of isolated bovine nasal cartilage explants (IC50 = 31 nM). It shows high selectivity (>1000 fold) for MMP-13 over other MMPs. In vivo, BI 4394 decreases the mean arthritic score vs control in a murine model of rheumatoid arthritis, when administered at a dose of 100 mg/kg over a 14-day period. BI 4394 is orally bioavailable.
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the BI 4394 page on the SGC website.
分子量 | 446.46 |
公式 | C24H22N4O5 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1222173-37-6 |
PubChem ID | 45376872 |
InChI Key | MMJPVSDTLGFIQW-UHFFFAOYSA-N |
Smiles | O=C(O)C1=CC=C(C=C1)CNC(=O)C2=NN(C(=C2)C=3C=CC=4NC(=CC4C3)C(=O)OCC)C |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 44.65 | 100 |
以下数据基于产品分子量 446.46。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.24 mL | 11.2 mL | 22.4 mL |
5 mM | 0.45 mL | 2.24 mL | 4.48 mL |
10 mM | 0.22 mL | 1.12 mL | 2.24 mL |
50 mM | 0.04 mL | 0.22 mL | 0.45 mL |
参考文献是支持产品生物活性的出版物。
Taylor et al (2011) Fragment-based discovery of indole inhibitors of matrix metalloproteinase-13. J.Med.Chem. 54 8174 PMID: 22017539
Taylor et al (2021) Indole inhibitors of MMP-13 for arthritic disorders. ACS Omega 6 18635 PMID: 34337203
If you know of a relevant reference for BI 4394, please let us know.
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