MMP13-IN-2 |
カタログ番号GC65957 |
MMP13-IN-2 は、強力で選択的な経口活性 MMP-13 阻害剤です。 MMP13-IN-2 は、MMP-1、3、7、8、9、14、および TACE よりも MMP-13 に対して優れた効力 (IC50 = 0.036 nM) と選択性 (1,500 倍以上) を示します。 MMP13-IN-2 は、軟骨からのコラーゲンの放出を in vitro でブロックする能力があります。 MMP13-IN-2 は、コラゲナーゼ関連疾患研究の可能性を秘めています。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 935759-55-0
Sample solution is provided at 25 µL, 10mM.
MMP13-IN-2 is a potent, selective and orally active MMP-13 inhibitor. MMP13-IN-2 exhibits excellent potency for MMP-13 (IC50=0.036 nM) and selectivities (greater than 1,500-fold) over MMP-1, 3, 7, 8, 9, 14, and TACE. MMP13-IN-2 has the ability to block the release of collagen from cartilage in vitro. MMP13-IN-2 has the potential for collagenase related disease research[1].
In a bovine nasal cartilage (BNC) assay, the chondrocyte-mediated degradation of cartilage was studied using bovine nasal cartilage slices cultured for up to 14 days. MMP13-IN-2 (0.01-1 µM) is effective at preventing the IL-1/OSM induced in vitro degradation of BNC (-17.6%, 48.4% and 70.8% inhibition of cartilage degradation, respectively).[1].
MMP13-IN-2 (oral gavage; 1 mg/kg) shows the best combination of CYP3A4 inhibition risk and oral exposure at a dose of 1 mg/kg in rats and mice (F% = 33 and 38, respectively)[1].
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