| Name | MMP13-IN-3 |
| Description | MMP13-IN-3 is >1000 selective over other MMPs. MMP13-IN-3 is an effective, selective, and orally active MMP-13 inhibitor (IC50=1 nM) for the potential treatment of osteoarthritis. |
| In vitro | MMP13-IN-3 inhibits MMP-2, MMP-9, MMP-10 and MMP-14 with IC50s of 18, 8.9, 16 and 8.3 μM, respectively. MMP13-IN-3 is effective in a full-length MMP-13 collagen degradation assay (11 nM) and is able to inhibit the degradation of bovine nasal cartilage (IC50: 31 nM) [1]. |
| In vivo | MMP13-IN-3 has short terminal elimination half-life (t1/2=0.47 h for rat (1 mg/kg, i.v.) and rat (10 mg/kg, orally), respectively). MMP13-IN-3 reaches micromolar plasma levels (AUC=1109±64 nM h/mL) when dosed orally at 10 mg/kg or i.v. 1 mg/kg. It displays modest clearance (CL=34 mL/min/kg), and shows acceptable bioavailability (39%). The Vss is quite low at 0.26 mL/mi/kg rat pharmacokinetic profile [1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 100 mg/mL (223.98 mM), Sonication and heating to 60℃ are recommended.
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| Keywords | inhibit | osteoarthritis | Inhibitor | MMP13 IN 3 | Matrix metalloproteinases | MMP-13-IN-3 | MMP13IN3 | MMP | MMP-13 | MMP13-IN-3 |
| Inhibitors Related | Stigmasterol | Ethyl gallate | Doxycycline (hyclate) | Chondroitin sulfate | Astragaloside IV | Doxycycline | Edaravone | Glucosamine | Triolein | Arctigenin | Fenofibric acid | Glucosamine sulfate |
| Related Compound Libraries | Bioactive Compound Library | Protease Inhibitor Library | Inhibitor Library | Anti-Fibrosis Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max |
United States
