MAGL-IN-5 (CAY10499) is a non-selective lipase inhibitor (antagonist) with IC50s for recombinant human monoacylglycerol lipase (MAGL), hormone-sensitive lipase (HSL) and fatty acid amide hydrolase (FAAH). 144, 90 and 14 nM respectively.

Physicochemical Properties

Molecular Formula	C18H17N3O5
Molecular Weight	355.35
Exact Mass	355.116
CAS #	359714-55-9
PubChem CID	9924775
Appearance	Off-white to yellow solid powder
Density	1.3±0.1 g/cm3
Index of Refraction	1.610
LogP	1.97
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	6
Heavy Atom Count	26
Complexity	547
Defined Atom Stereocenter Count	0
InChi Key	QTENHWTVRQKWRI-UHFFFAOYSA-N
InChi Code	InChI=1S/C18H17N3O5/c1-12-10-14(21-18(23)26-17(20-21)24-2)8-9-15(12)19-16(22)25-11-13-6-4-3-5-7-13/h3-10H,11H2,1-2H3,(H,19,22)
Chemical Name	benzyl N-[4-(5-methoxy-2-oxo-1,3,4-oxadiazol-3-yl)-2-methylphenyl]carbamate
Synonyms	CAY 10499; CAY-10499; CAY10499
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

References	[1]. CAY10499, a novel monoglyceride lipase inhibitor evidenced by an expeditious MGL assay. Chembiochem. 2008 Nov 3;9(16):2704-10. [2]. 4-Aryliden-2-methyloxazol-5(4H)-one as a new scaffold for selective reversible MAGL inhibitors. J Enzyme Inhib Med Chem. 2016;31(1):137-46.
Additional Infomation	CAY10499 is a carbamate ester.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~281.42 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (7.04 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.8141 mL	14.0706 mL	28.1413 mL
	5 mM	0.5628 mL	2.8141 mL	5.6283 mL
	10 mM	0.2814 mL	1.4071 mL	2.8141 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.