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URB602

Name: URB602
Brand: TargetMol
SKU: T3591
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3591Cas No. 565460-15-3

URB602 is a specific monoacylglycerol lipase (MGL) inhibitor, which inhibits rat brain MGL (IC50: 28±4 μM) through a noncompetitive mechanism.

URB602

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Purity: 99.9%

Catalog No. T3591Cas No. 565460-15-3

URB602 is a specific monoacylglycerol lipase (MGL) inhibitor, which inhibits rat brain MGL (IC50: 28±4 μM) through a noncompetitive mechanism.

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$38	In Stock	In Stock
50 mg	$68	In Stock	In Stock
100 mg	$119	In Stock	In Stock
200 mg	$175	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$29	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.9%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	URB602 is a specific monoacylglycerol lipase (MGL) inhibitor, which inhibits rat brain MGL (IC50: 28±4 μM) through a noncompetitive mechanism.
Targets&IC50	MGL:28±4 μM
In vitro	The apparent Km of MGL for 2-AG is 24±1.7 μM and the Vmax is 1814±51 nmol/min/mg protein; with URB602, the Km is 20±0.4 μM and the Vmax is 541±20 nmol/min/mg protein (n=4). When organotypic slice cultures of rat forebrain are incubated with URB602 (100 μM), both baseline and Ca2+-ionophore-stimulated 2-arachidonoylglycerol (2-AG) concentrations are increased[1]. URB602 weakly inhibits recombinant MGL (IC50: 223±63 μM) through a rapid and noncompetitive mechanism.
In vivo	URB602 (20-40 mg/kg) can reduce upper GI transit and slow colonic propulsion. In whole gut transit, URB602 dose-dependently inhibits transit (P<0.05) compared with the vehicle control group. The inhibitory action of URB602 (40 mg/kg) on whole gut transit is absent in these mice, demonstrating CB1 receptor involvement in the inhibitory action[3]. During the early phase of the formalin test, URB602 decreases the AUC of pain behavior for JZL184 (ED50: 0.06±0.028 μg) and for URB602 (ED50: 120±51.3 μg) in adult male Sprague-Dawley rats. Both MGL inhibitors also suppress pain behavior during the late phase of formalin pain for JZL184 (ED50: 0.03±0.011 μg) and for URB602 (ED50: 66±23.9 μg).
Kinase Assay	Samples containing either URB602 (300 μM), MGL (1.4 pM), or both URB602 and MGL are incubated at 37°C for 30 min in assay buffer. At various time points, the reaction is stopped with an equal volume of ice-cold methanol and directly analyzed in positive ionization mode by LC/MS. A SB-CN column (150×2.1 mm i.d., 5 μm) eluted is used with a linear gradient of methanol in water containing 0.25% acetic acid and 5 mM ammonium acetate (from 60% to 100% of methanol in 8 min) at a flow rate of 0.5 mL/min with column temperature at 50°C. Capillary voltage is set at 4 kV and fragmentor voltage is 100V. Nebulizer pressure is set at 60 psi. N2 is used as drying gas at a flow rate of 13 liters/min and a temperature of 350°C. ESI is in the positive mode and a full scan spectrum is acquired from m/z 100 to 600. Extracted ion chromatograms are used to quantify URB602 ([M+H]+, m/z 296)[2].

Chemical Properties

Molecular Weight	295.38
Formula	C₁₉H₂₁NO₂
Cas No.	565460-15-3
Smiles	O=C(Nc1cccc(c1)-c1ccccc1)OC1CCCCC1
Relative Density.	1.149g/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.

Solubility Information

DMSO: 55 mg/mL (186.2 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 2.5 mg/mL (8.46 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.3855 mL	16.9273 mL	33.8547 mL	169.2735 mL
5 mM	0.6771 mL	3.3855 mL	6.7709 mL	33.8547 mL
10 mM	0.3385 mL	1.6927 mL	3.3855 mL	16.9273 mL
20 mM	0.1693 mL	0.8464 mL	1.6927 mL	8.4637 mL
50 mM	0.0677 mL	0.3385 mL	0.6771 mL	3.3855 mL
100 mM	0.0339 mL	0.1693 mL	0.3385 mL	1.6927 mL

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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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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