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MMP13-IN-3

🥰Excellent
Catalog No. T16124Cas No. 1222173-37-6

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.

MMP13-IN-3

MMP13-IN-3

🥰Excellent
Purity: 99.05%
Catalog No. T16124Cas No. 1222173-37-6
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.
Pack SizePriceAvailabilityQuantity
1 mg$89In Stock
5 mg$228In Stock
10 mg$372In Stock
25 mg$653In Stock
50 mg$892In Stock
100 mg$1,230In Stock
1 mL x 10 mM (in DMSO)$253In Stock
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Purity:99.05%
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Product Introduction

Bioactivity
Description
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.
Targets&IC50
MMP2:18 μM, MMP13:1 nM, MMP9:8.9 μM, MMP10:16 μM, MMP14:8.3 μM
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) [1].
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 [1].
Chemical Properties
Molecular Weight446.46
FormulaC24H22N4O5
Cas No.1222173-37-6
SmilesCCOC(=O)c1cc2cc(ccc2[nH]1)-c1cc(nn1C)C(=O)NCc1ccc(cc1)C(O)=O
Relative Density.1.38 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 100 mg/mL (223.98 mM), Sonication and heating to 60℃ are recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2398 mL11.1992 mL22.3984 mL111.9921 mL
5 mM0.4480 mL2.2398 mL4.4797 mL22.3984 mL
10 mM0.2240 mL1.1199 mL2.2398 mL11.1992 mL
20 mM0.1120 mL0.5600 mL1.1199 mL5.5996 mL
50 mM0.0448 mL0.2240 mL0.4480 mL2.2398 mL
100 mM0.0224 mL0.1120 mL0.2240 mL1.1199 mL

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