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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $89 | In Stock | |
5 mg | $228 | In Stock | |
10 mg | $372 | In Stock | |
25 mg | $653 | In Stock | |
50 mg | $892 | In Stock | |
100 mg | $1,230 | In Stock | |
1 mL x 10 mM (in DMSO) | $253 | In Stock |
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. |
Targets&IC50 | MMP2:18 μM, MMP13:1 nM, MMP9:8.9 μM, MMP10:16 μM, MMP14:8.3 μM |
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]. |
Molecular Weight | 446.46 |
Formula | C24H22N4O5 |
Cas No. | 1222173-37-6 |
Smiles | CCOC(=O)c1cc2cc(ccc2[nH]1)-c1cc(nn1C)C(=O)NCc1ccc(cc1)C(O)=O |
Relative Density. | 1.38 g/cm3 (Predicted) |
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. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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