MMP13-IN-2

Name: MMP13-IN-2
Brand: TargetMol
SKU: T41079
Rating: 4.5 (1 reviews)

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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

🥰Excellent

Catalog No. T41079Alias MMP13-IN-2Cas No. 935759-55-0

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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	MMP2:180 nM (IC50), MMP13:0.036 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].
Synonyms	MMP13-IN-2

Chemical Properties

Molecular Weight	506.51
Formula	C₂₄H₁₉FN₆O₄S
Cas No.	935759-55-0
Smiles	Fc1cccc(c1)-c1csc2[nH]c(nc(=O)c12)C(=O)NCc1cccc(OCCOc2ncn[nH]2)c1
Relative Density.	1.53 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc