Cat. No.: HY-119283

CAY10499

(Synonyms: MAGL-IN-5)

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

CAY10499 (MAGL-IN-5) is a non-selective lipase inhibitor with IC₅₀ values of 144 nM and 14 nM for monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH), respectively. Additionally, CAY10499 exhibits anti-inflammatory and antiviral activities.

For research use only. We do not sell to patients.

Purity: 99.58%
CAS No.: 359714-55-9
Formula: C₁₈H₁₇N₃O₅
Molecular Weight:355.34

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

CAY10499 Chemical Structure

CAS No.: 359714-55-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
Caov-3 cell line	IC₅₀	77 μM Compound: CAY10499	Antiproliferative activity against human Caov3 cells after 96 hrs Antiproliferative activity against human Caov3 cells after 96 hrs	[PMID: 29309142]
Caov-3 cell line	IC₅₀	83.1 μM Compound: 2; CAY10499	Antiproliferative activity against human Caov-3 cells assessed as reduction in cell viability incubated for 96 hrs by Cell-titer-Glo luminescent cell viability assay Antiproliferative activity against human Caov-3 cells assessed as reduction in cell viability incubated for 96 hrs by Cell-titer-Glo luminescent cell viability assay	[PMID: 27809504]
Caov-3 cell line	IC₅₀	92 μM Compound: 2; CAY10499	Growth inhibition of human Caov3 cells after 96 hrs by celltiter-glo assay Growth inhibition of human Caov3 cells after 96 hrs by celltiter-glo assay	[PMID: 30715876]
Caov-3 cell line	IC₅₀	92 μM Compound: CAY10499; 2	Antiproliferative activity against human Caov3 cells measured after 96 hrs Antiproliferative activity against human Caov3 cells measured after 96 hrs	[PMID: 30144699]
Caov-3 cell line	IC₅₀	95 μM Compound: CAY10499;2	Antiproliferative activity against human CAOV3 cells as reduction in cell growth measured after 96 hrs by Celltiter-glo luminescent assay Antiproliferative activity against human CAOV3 cells as reduction in cell growth measured after 96 hrs by Celltiter-glo luminescent assay	[PMID: 33045662]
HCT-116	IC₅₀	38 μM Compound: CAY10499;2	Antiproliferative activity against human HCT116 cells as reduction in cell growth measured after 96 hrs by Celltiter-glo luminescent assay Antiproliferative activity against human HCT116 cells as reduction in cell growth measured after 96 hrs by Celltiter-glo luminescent assay	[PMID: 33045662]
HCT-116	IC₅₀	42 μM Compound: 2; CAY10499	Growth inhibition of human HCT116 cells after 96 hrs by celltiter-glo assay Growth inhibition of human HCT116 cells after 96 hrs by celltiter-glo assay	[PMID: 30715876]
HCT-116	IC₅₀	89 μM Compound: CAY10499; 2	Antiproliferative activity against human HCT116 cells measured after 96 hrs Antiproliferative activity against human HCT116 cells measured after 96 hrs	[PMID: 30144699]
MCF7	IC₅₀	4.2 μM Compound: CAY10499	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 96 hrs Cytotoxicity against human MCF7 cells assessed as growth inhibition after 96 hrs	[PMID: 24853323]
MDA-MB-231	IC₅₀	42 μM Compound: CAY10499; 2	Antiproliferative activity against human MDA-MB-231 cells measured after 96 hrs Antiproliferative activity against human MDA-MB-231 cells measured after 96 hrs	[PMID: 30144699]
MDA-MB-231	IC₅₀	46 μM Compound: CAY10499	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 96 hrs Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 96 hrs	[PMID: 24853323]
MDA-MB-231	IC₅₀	83 μM Compound: CAY10499;2	Antiproliferative activity against human MDA-MB-231 cells as reduction in cell growth measured after 96 hrs by Celltiter-glo luminescent assay Antiproliferative activity against human MDA-MB-231 cells as reduction in cell growth measured after 96 hrs by Celltiter-glo luminescent assay	[PMID: 33045662]
MDA-MB-231	IC₅₀	89 μM Compound: 2; CAY10499	Growth inhibition of human MDA-MB-231 cells after 96 hrs by celltiter-glo assay Growth inhibition of human MDA-MB-231 cells after 96 hrs by celltiter-glo assay	[PMID: 30715876]
MRC5	IC₅₀	>100 μM Compound: 2; CAY10499	Growth inhibition of human MRC5 cells after 96 hrs by celltiter-glo assay Growth inhibition of human MRC5 cells after 96 hrs by celltiter-glo assay	[PMID: 30715876]
MRC5	IC₅₀	>100 μM Compound: CAY10499	Antiproliferative activity against human MRC5 cells after 96 hrs Antiproliferative activity against human MRC5 cells after 96 hrs	[PMID: 29309142]
MRC5	IC₅₀	>200 μM Compound: 2; CAY10499	Antiproliferative activity against human MRC5 cells assessed as reduction in cell viability incubated for 96 hrs by Cell-titer-Glo luminescent cell viability assay Antiproliferative activity against human MRC5 cells assessed as reduction in cell viability incubated for 96 hrs by Cell-titer-Glo luminescent cell viability assay	[PMID: 27809504]
OVCAR-3	IC₅₀	>79.8 μM Compound: CAY10499	Cytotoxicity against human OVCAR3 cells assessed as growth inhibition after 96 hrs Cytotoxicity against human OVCAR3 cells assessed as growth inhibition after 96 hrs	[PMID: 24853323]
OVCAR-3	IC₅₀	43 μM Compound: CAY10499	Antiproliferative activity against human OVCAR3 cells after 96 hrs Antiproliferative activity against human OVCAR3 cells after 96 hrs	[PMID: 29309142]
OVCAR-3	IC₅₀	45 μM Compound: 2; CAY10499	Antiproliferative activity against human OVCAR-3 cells assessed as reduction in cell viability incubated for 96 hrs by Cell-titer-Glo luminescent cell viability assay Antiproliferative activity against human OVCAR-3 cells assessed as reduction in cell viability incubated for 96 hrs by Cell-titer-Glo luminescent cell viability assay	[PMID: 27809504]
OVCAR-3	IC₅₀	50 μM Compound: 2; CAY10499	Growth inhibition of human OVCAR3 cells after 96 hrs by celltiter-glo assay Growth inhibition of human OVCAR3 cells after 96 hrs by celltiter-glo assay	[PMID: 30715876]
OVCAR-3	IC₅₀	50 μM Compound: CAY10499; 2	Antiproliferative activity against human OVCAR3 cells measured after 96 hrs Antiproliferative activity against human OVCAR3 cells measured after 96 hrs	[PMID: 30144699]
OVCAR-3	IC₅₀	53 μM Compound: CAY10499;2	Antiproliferative activity against human OVCAR3 cells as reduction in cell growth measured after 96 hrs by Celltiter-glo luminescent assay Antiproliferative activity against human OVCAR3 cells as reduction in cell growth measured after 96 hrs by Celltiter-glo luminescent assay	[PMID: 33045662]
SK-OV-3	IC₅₀	33 μM Compound: CAY10499;2	Antiproliferative activity against human SKOV3 cells as reduction in cell growth measured after 96 hrs by Celltiter-glo luminescent assay Antiproliferative activity against human SKOV3 cells as reduction in cell growth measured after 96 hrs by Celltiter-glo luminescent assay	[PMID: 33045662]
SK-OV-3	IC₅₀	34 μM Compound: 2; CAY10499	Growth inhibition of human SKOV3 cells after 96 hrs by celltiter-glo assay Growth inhibition of human SKOV3 cells after 96 hrs by celltiter-glo assay	[PMID: 30715876]
SK-OV-3	IC₅₀	34 μM Compound: CAY10499; 2	Antiproliferative activity against human SKOV3 cells measured after 96 hrs Antiproliferative activity against human SKOV3 cells measured after 96 hrs	[PMID: 30144699]

In Vitro

CAY10499 (20 mg/L; 42-44 h) can inhibit the maturation of oocytes, increase the triglyceride content in mature oocytes, and reduce the mitochondrial membrane potential^[1].
CAY10499 (20 μM; 12-18 h) exhibits antiviral and anti-inflammatory activities in SARS-CoV-2-infected Vero E6 cells and IAV-infected A549 cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR^[2]

Cell Line:

SARS-CoV-2-infected Vero E6 cells
Concentration:

20 μM
Incubation Time:

12 and 18 h
Result:

Markedly reduced levels of TNF-α, IL-6, and MCP-1.

In Vivo

CAY10499 (intraperitoneal injection; 0.01-10 mg/kg; twice daily; 4 days) exhibits protective and antiviral activities in a mouse model infected with IAV, and can improve the survival rate of mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 359714-55-9
Appearance Solid
Molecular Weight 355.34
Formula C₁₈H₁₇N₃O₅
Color Off-white to yellow
SMILES

O=C(OCC1=CC=CC=C1)NC2=CC=C(N3C(OC(OC)=N3)=O)C=C2C
Synonyms

MAGL-IN-5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (1)

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Journal Impact Factor

Nat Commun

Phosphorylation of 17β-hydroxysteroid dehydrogenase 13 at serine 33 attenuates nonalcoholic fatty liver disease in mice. [Abstract]

2022 Nov 2;13(1):6577. PMID: 36323699

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (281.42 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8142 mL

14.0710 mL

28.1421 mL

5 mM

0.5628 mL

2.8142 mL

5.6284 mL

10 mM

0.2814 mL

1.4071 mL

2.8142 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Zhuan Q, et al. Cytoplasm lipids can be modulated through hormone-sensitive lipase and are related to mitochondrial function in porcine IVM oocytes. Reprod Fertil Dev. 2020 Apr;32(7):667-675. [Content Brief]

[2]. Baek YB, et al. Therapeutic strategy targeting host lipolysis limits infection by SARS-CoV-2 and influenza A virus. Signal Transduct Target Ther. 2022 Oct 17;7(1):367. [Content Brief]

[3]. Muccioli GG, et al. CAY10499, a novel monoglyceride lipase inhibitor evidenced by an expeditious MGL assay. Chembiochem. 2008 Nov 3;9(16):2704-10. [Content Brief]

[4]. Granchi C, et al. 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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8142 mL	14.0710 mL	28.1421 mL	70.3552 mL
	5 mM	0.5628 mL	2.8142 mL	5.6284 mL	14.0710 mL
	10 mM	0.2814 mL	1.4071 mL	2.8142 mL	7.0355 mL
	15 mM	0.1876 mL	0.9381 mL	1.8761 mL	4.6903 mL
	20 mM	0.1407 mL	0.7036 mL	1.4071 mL	3.5178 mL
	25 mM	0.1126 mL	0.5628 mL	1.1257 mL	2.8142 mL
	30 mM	0.0938 mL	0.4690 mL	0.9381 mL	2.3452 mL
	40 mM	0.0704 mL	0.3518 mL	0.7036 mL	1.7589 mL
	50 mM	0.0563 mL	0.2814 mL	0.5628 mL	1.4071 mL
	60 mM	0.0469 mL	0.2345 mL	0.4690 mL	1.1726 mL
	80 mM	0.0352 mL	0.1759 mL	0.3518 mL	0.8794 mL
	100 mM	0.0281 mL	0.1407 mL	0.2814 mL	0.7036 mL

Keywords

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CAY10499

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Neuronal Signaling Compound Library

Antiviral Compound Library

Anti-Cancer Metabolism Compound Library

Lipid Metabolism Compound Library

Pain-Related Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) CAY10499

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

CAY10499

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Neuronal Signaling Compound Library

Antiviral Compound Library

Anti-Cancer Metabolism Compound Library

Lipid Metabolism Compound Library

Pain-Related Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) CAY10499

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

CAY10499 Related Classifications

HY-119283 Related Classifications