CAY10499 (Synonyms: MAGL-IN-5)

Name: CAY10499
Brand: MedChemExpress
SKU: HY-119283
Rating: 4.5 (1 reviews)

Cat. No.: HY-119283 Purity: 99.58%: Data Sheet
SDS

COA
Handling Instructions Technical Support

Solubility

In Vivo Dissolution Calculator

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.

CAY10499 Chemical Structure

CAS No. : 359714-55-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE CAY10499

•Nat Commun. 2022 Nov 2;13(1):6577. [Abstract]

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Biological Activity
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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.

Molecular Weight

355.34

Formula

C₁₈H₁₇N₃O₅

CAS No.

359714-55-9

Appearance

Solid

Color

Off-white to yellow

SMILES

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

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)

Solvent & Solubility

In Vitro:

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

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Purity & Documentation

Purity: 99.58%

Select Batch:

Data Sheet (274 KB) SDS (252 KB)

COA (247 KB) HNMR (262 KB) LCMS (95 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]

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

CAY10499 Related Classifications

Metabolic Disease Inflammation/Immunology Infection

Keywords:

CAY10499359714-55-9MAGL-IN-5CAY 10499CAY-10499MAGLFAAHSARS-CoVInfluenza VirusMonoacylglycerol lipaseFatty acid amide hydrolaseSARS coronavirusoocytesVero E6 cellsA549 cellsInhibitorinhibitorinhibit

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CAY10499 (Synonyms: MAGL-IN-5)

Customer Review

1 Publications Citing Use of MCE CAY10499

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•Related Screening Libraries:

Biological Activity

Purity & Documentation

References

Customer Review

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Complete Stock Solution Preparation Table

CAY10499 Related Classifications

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