| Identification | Back Directory | [Name]
BI-4394
(BI4394) | [CAS]
1222173-37-6 | [Synonyms]
MMP13-IN-3
BI-4394
(BI4394)
inhibit,osteoarthritis,Inhibitor,MMP13 IN 3,Matrix metalloproteinases,MMP-13-IN-3,MMP13IN3,MMP,MMP-13 | [Molecular Formula]
C24H22N4O5 | [MDL Number]
MFCD34567262 | [MOL File]
1222173-37-6.mol | [Molecular Weight]
446.46 |
| Chemical Properties | Back Directory | [Boiling point ]
764.4±60.0 °C(Predicted) | [density ]
1.38±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (223.98 mM; ultrasonic and warming and heat to 60°C) | [form ]
A solid | [pka]
4.16±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
MMP13-IN-3 is a potent and orally active matrix metalloproteinase-13 (MMP-13) inhibitor for the potential treatment of osteoarthritis and other related arthritic diseases. | [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 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)[1]. | Animal Model: | Srapgue Dally Rats[1] | | 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. |
| [IC 50]
MMP-13: 1 nM (IC50); MMP-14: 8.3 μM (IC50); MMP-9: 8.9 μM (IC50); MMP-10: 16 μM (IC50); MMP-2: 18 μM (IC50) | [storage]
Store at -20°C |
|
| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
|