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MMP13-IN-2

🥰Excellent
Catalog No. T41079Cas No. 935759-55-0
Alias MMP13-IN-2

MMP13-IN-2 is a highly potent, selective, and orally active inhibitor of MMP-13. It demonstrates exceptional potency against MMP-13, with an IC50 value of 0.036 nM, and exhibits selectivities greater than 1,500-fold over MMP-1, 3, 7, 8, 9, 14, and TACE. Moreover, MMP13-IN-2 possesses the capability to effectively inhibit collagen release from cartilage in vitro. Consequently, MMP13-IN-2 holds great potential for advancing research on collagenase-related diseases.

MMP13-IN-2

MMP13-IN-2

🥰Excellent
Catalog No. T41079Alias MMP13-IN-2Cas No. 935759-55-0
MMP13-IN-2 is a highly potent, selective, and orally active inhibitor of MMP-13. It demonstrates exceptional potency against MMP-13, with an IC50 value of 0.036 nM, and exhibits selectivities greater than 1,500-fold over MMP-1, 3, 7, 8, 9, 14, and TACE. Moreover, MMP13-IN-2 possesses the capability to effectively inhibit collagen release from cartilage in vitro. Consequently, MMP13-IN-2 holds great potential for advancing research on collagenase-related diseases.
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Product Introduction

Bioactivity
Description
MMP13-IN-2 is a highly potent, selective, and orally active inhibitor of MMP-13. It demonstrates exceptional potency against MMP-13, with an IC50 value of 0.036 nM, and exhibits selectivities greater than 1,500-fold over MMP-1, 3, 7, 8, 9, 14, and TACE. Moreover, MMP13-IN-2 possesses the capability to effectively inhibit collagen release from cartilage in vitro. Consequently, MMP13-IN-2 holds great potential for advancing research on collagenase-related diseases.
Targets&IC50
MMP13:0.036 nM (IC50), MMP2:180 nM (IC50), MMP3:1100 nM (IC50)
In vitro
In a study examining chondrocyte-mediated degradation of cartilage, bovine nasal cartilage (BNC) slices were cultured for up to 14 days. The compound MMP13-IN-2, at concentrations ranging from 0.01 to 1 μM, was found to effectively inhibit the IL-1/OSM-induced degradation of BNC in vitro, with inhibition percentages of -17.6%, 48.4%, and 70.8%, respectively.[1].
In vivo
MMP13-IN-2, administered via oral gavage at a dose of 1 mg/kg, demonstrates an optimal balance between the risk of CYP3A4 inhibition and oral bioavailability in both rats and mice, with bioavailability percentages (F%) of 33 and 38, respectively[1].
AliasMMP13-IN-2
Chemical Properties
Molecular Weight506.51
FormulaC24H19FN6O4S
Cas No.935759-55-0
Relative Density.1.53 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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Keywords

MMP13IN2MMP13 IN 2MMP-13-IN-2
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