Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MMP13-IN-2 is a highly potent, selective, and orally active inhibitor of MMP-13. It demonstrates exceptional potency against MMP-13, with an IC50 value of 0.036 nM, and exhibits selectivities greater than 1,500-fold over MMP-1, 3, 7, 8, 9, 14, and TACE. Moreover, MMP13-IN-2 possesses the capability to effectively inhibit collagen release from cartilage in vitro. Consequently, MMP13-IN-2 holds great potential for advancing research on collagenase-related diseases.
説明 | MMP13-IN-2 is a highly potent, selective, and orally active inhibitor of MMP-13. It demonstrates exceptional potency against MMP-13, with an IC50 value of 0.036 nM, and exhibits selectivities greater than 1,500-fold over MMP-1, 3, 7, 8, 9, 14, and TACE. Moreover, MMP13-IN-2 possesses the capability to effectively inhibit collagen release from cartilage in vitro. Consequently, MMP13-IN-2 holds great potential for advancing research on collagenase-related diseases. |
ターゲット&IC50 | MMP2:180 nM (IC50), MMP13:0.036 nM (IC50), MMP3:1100 nM (IC50) |
In vitro | In a study examining chondrocyte-mediated degradation of cartilage, bovine nasal cartilage (BNC) slices were cultured for up to 14 days. The compound MMP13-IN-2, at concentrations ranging from 0.01 to 1 μM, was found to effectively inhibit the IL-1/OSM-induced degradation of BNC in vitro, with inhibition percentages of -17.6%, 48.4%, and 70.8%, respectively.[1]. |
In vivo | MMP13-IN-2, administered via oral gavage at a dose of 1 mg/kg, demonstrates an optimal balance between the risk of CYP3A4 inhibition and oral bioavailability in both rats and mice, with bioavailability percentages (F%) of 33 and 38, respectively[1]. |
別名 | MMP13-IN-2 |
分子量 | 506.51 |
分子式 | C24H19FN6O4S |
CAS No. | 935759-55-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. 詳細
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MMP13-IN-2 935759-55-0 MMP13IN2 MMP13 IN 2 MMP-13-IN-2 Inhibitor inhibitor inhibit