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BI-4394

CAS No. : 1222173-37-6

產(chǎn)品活性：BI-4394 (MMP13-IN-3) is a potent, selective, and orally active MMP-13 inhibitor (IC₅₀=1 nM) for the potential treatment of osteoarthritis. BI-4394 is >1000 selective over other MMPs.

研究領(lǐng)域：Metabolic Enzyme/Protease

作用靶點(diǎn)：MMP

In Vitro: BI-4394 (Compound 15) is potent in a full-length MMP-13 collagen degradation assay (11 nM) and is able to inhibit degradation of bovine nasal cartilage with an IC₅₀ of 31 nM. BI-4394 inhibits MMP-2, MMP-9, MMP-10 and MMP-14 with IC₅₀s of 18, 8.9, 16 and 8.3 μM, respectively.

In Vivo: When dosed orally at 10 mg/kg or i.v. 1 mg/kg, BI-4394 (Compound 15) reaches micromolar plasma levels (AUC=1109±64 nM h/mL), displays modest clearance (CL=34 mL/min/kg), and shows acceptable bioavailability (39%). The V_ss is quite low at 0.26 mL/mi/kg rat pharmacokinetic profile. BI-4394 has short terminal elimination half-life (t_1/2=0.47 h for rat (1 mg/kg, i.v.) and rat (10 mg/kg, orally), respectively).

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