| Chemical Properties | Back Directory | [density ]
1.53±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (197.43 mM; ultrasonic and warming and heat to 60°C) | [form ]
Solid | [pka]
9.09±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
MMP13-IN-2 is a potent, selective and orally active MMP-13 inhibitor. MMP13-IN-2 exhibits excellent potency for MMP-13 (IC50=0.036 nM) and selectivities (greater than 1,500-fold) over MMP-1, 3, 7, 8, 9, 14, and TACE. MMP13-IN-2 has the ability to block the release of collagen from cartilage in vitro. MMP13-IN-2 has the potential for collagenase related disease research[1]. | [in vivo]
MMP13-IN-2 (oral gavage; 1 mg/kg) shows the best combination of CYP3A4 inhibition risk and oral exposure at a dose of 1 mg/kg in rats and mice (F% = 33 and 38, respectively)[1]. | [IC 50]
MMP-13: 0.036 nM (IC50); MMP-2: 180 nM (IC50); MMP-3: 1100 nM (IC50) | [storage]
Store at -20°C | [References]
[1] Hiroshi Nara, et al. Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach. J Med Chem. 2017 Jan 26;60(2):608-626. DOI:10.1021/acs.jmedchem.6b01007 |
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