MMP13-IN-3

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MMP13-IN-3 比其他 MMP 的选择性 >1000。 MMP13-IN-3 是一种有效的、选择性的、口服活性的 MMP-13 抑制剂 (IC50=1 nM)，可用于治疗骨关节炎。

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) .(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 .

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.

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 Vss is quite low at 0.26 mL/mi/kg rat pharmacokinetic profile. BI-4394 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). Animal Model:Srapgue Dally Rats Dosage:10 mg/kg (oral gavage); 1 mg/kg (i.v.)Administration:Dosed orally (10 mg/kg); i.v. (1 mg/kg)(Pharmacokinetic Analysis)Result:T1/2=0.47 h for rat (1 mg/kg, i.v.) and rat (10 mg/kg, orally) , respectively.

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Metabolic Enzyme/Protease

MMP

DNA/RNA Synthesis| Nucleoside Antimetabolite/Analog

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1222173-37-6

446.463

C24H22N4O5

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (223.98 mM)

CCOC(=O)c1cc2cc(ccc2[nH]1)-c1cc(nn1C)C(=O)NCc1ccc(cc1)C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years