产品
编 号：F080866
分子式：C24H22N4O5
分子量：446.46
分子式：C24H22N4O5
分子量：446.46
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 1222173-37-6
产品详情
生物活性：
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.
体内研究：
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.
体外研究：
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.
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.
体内研究：
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.
体外研究：
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.
产品资料
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