UK-370106

Name: UK-370106
Brand: TargetMol
SKU: T13249
Rating: 4.5 (1 reviews)

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Catalog No. T13249Cas No. 230961-21-4

UK-370106 is a potent and highly selective inhibitor of MMP-3 (IC50: 23 nM) and MMP-12 (IC50: 42 nM), effectively inhibiting the cleavage of [3H]-fibronectin by MMP-3 (IC50: 320 nM).

UK-370106

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Catalog No. T13249Cas No. 230961-21-4

UK-370106 is a potent and highly selective inhibitor of MMP-3 (IC50: 23 nM) and MMP-12 (IC50: 42 nM), effectively inhibiting the cleavage of [3H]-fibronectin by MMP-3 (IC50: 320 nM).

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
10 mg	$1,120	35 days	35 days

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Product Introduction

Bioactivity

Description	UK-370106 is a potent and highly selective inhibitor of MMP-3 (IC50: 23 nM) and MMP-12 (IC50: 42 nM), effectively inhibiting the cleavage of [3H]-fibronectin by MMP-3 (IC50: 320 nM).
Targets&IC50	MMP8:1.75 μM, MMP9:30.4 μM, MMP12:42 nM, MMP7:5.8 μM, MMP2:34.2 μM, MMP13:2.3 μM, MMP14:66.9 μM, MMP3:23 nM
In vitro	UK-370106 potency for the inhibition of MMP-13 is 2.3 μM, some 100-fold less potent than its inhibition of MMP-3. UK-370106 is found to be inactive (IC50 > 100 μM) vs zinc metalloproteases PCP and TACE and possesses the following inhibitory potencies vs MMP-2 (IC50 of 34.2 μM), MMP-7 (IC50 of 5.8 μM), MMP-8 (IC50 of 1.75 μM), MMP-9 (IC50 of 30.4 μM) and MMP-14 (IC50 of 66.9 μM)[1]. UK-370106 potently inhibits cleavage of [3H]-fibronectin by MMP-3 (IC50 of 320 nM)[1].
In vivo	Following intravenous (rat; 2 mg/kg) or topical administration to dermal wounds (rabbit), UK-370106 (compound 7) is rapidly cleared from plasma (t1/2 = 23 min) but slowly from dermal tissue (t1/2 approximately 3 days). Topical administration of UK-370106 for 6 days substantially inhibits MMP-3 ex vivo in a model of chronic dermal ulcers [1].

Chemical Properties

Molecular Weight	572.73
Formula	C₃₅H₄₄N₂O₅
Cas No.	230961-21-4
Smiles	CC1=C(C=CC(CCC[C@@H](C(N[C@H](C(N[C@H](COC)C2=CC=CC=C2)=O)C(C)(C)C)=O)CC(O)=O)=C1)C3=CC=CC=C3
Relative Density.	1.123g/cm3

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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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