AM9053
Based on 1 Customer Validation
AM9053 is a selective NAAA inhibitor. AM9053 inhibits NAAA catalytic activity, reduces N-acylethanolamine degradation and elevates PEA/OEA levels, indirectly activating PPAR-α and TRPV1, thereby exerting antiproliferative effects. AM9053 reduces LPS-induced nitrite production in microglia, counteracts colitis, and attenuates TNBS-induced intestinal fibrosis disease activity, collagen deposition, and fibrosis-related gene expression. AM9053 modulates macrophage polarization, macrophage-fibroblast crosstalk, T helper cell subset balance, IL-23/STAT3 signaling, and EMT-related genes. AM9053 inhibits colorectal cancer proliferation and migration, induces S phase arrest, downregulates cyclin A2/CDK2, and reduces xenograft tumor growth and azoxymethane-induced colon tumorigenesis. AM9053 can be used for research on colitis, intestinal fibrosis, and colorectal cancer.
For research use only. We do not sell to patients.
- Purity : 98.36%
- CAS No.: 157469-21-1
- Formula: C17H25NS
- Molecular Weight:275.45
-
Storage:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
|
PPARα |
TRPV1 |
IL-23 |
CDK2/cyclinE |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
1.056 μM
|
Antiproliferative activity against human HCT116 colon adenocarcinoma cells assessed by bromodeoxyuridine incorporation ELISA after 24 hrs exposure and 2 hrs incubation with 10 μM bromodeoxyuridine.
Antiproliferative activity against human HCT116 colon adenocarcinoma cells assessed by bromodeoxyuridine incorporation ELISA after 24 hrs exposure and 2 hrs incubation with 10 μM bromodeoxyuridine.
|
34791641 |
In Vitro
AM9053 (3 μM; 24 h) reduces the proliferation of Caco-2 colorectal cancer cells and inhibits the proliferation of HCEC healthy colonic epithelial cells[3].
AM9053 (3 μM; 24 h) reduces HCT116 proliferation through PPAR-α and TRPV1-dependent mechanisms[3].
AM9053 (3 μM; 24 h) reduces the migration of HCT116 and Caco-2 colorectal cancer cells in a PPAR-α/TRPV1-independent manner[3].
AM9053 reduces LPS-induced production of IL-23 and related cytokines in primary BMDMs[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HCT116 human colon adenocarcinoma cells, HCEC immortalized healthy human colonic epithelial cells
-
Concentration:0.1, 0.3, 1, and 3 μM
-
Incubation Time:24 h
-
Result:Did not exert cytotoxic effects on HCT116 cells and HCEC cells.
-
Cell Line:HCT116 human colon adenocarcinoma cells, Caco-2 human colon adenocarcinoma cells, HCEC immortalized healthy human colonic epithelial cells
-
Concentration:0.1, 0.3, 1, and 3 μM (HCT116)
3 μM (Caco-2, HCEC) -
Incubation Time:24 h
-
Result:Reduced HCT116 proliferation with an IC50 of 1.056 μM.
Produced 80.95% Caco-2 cell proliferation.
Did not affect the proliferation rate of HCEC cells.
-
Cell Line:HCT116 human colon adenocarcinoma cells
-
Concentration:3 μM
3 μM (GW6471 (HY-15372)); 0.1 μM (5′-iodoresiniferatoxin); 1 μM (AM251 (HY-15443)); 1 μM (AM630 (HY-12833)) -
Incubation Time:24 h
30 min (antagonists) -
Result:Reduced HCT116 proliferation through PPAR-α- and TRPV1-dependent mechanisms.
-
Cell Line:HCT116 human colon adenocarcinoma cells
-
Concentration:3 μM
-
Incubation Time:24 h
-
Result:Increased the percentage of cells in S phase and reduced the proportion of cells in G0/G1 phase; the representative density plot showed S phase 21.4%, G2/M 20.7%, and G0/G1 54.6%.
-
Cell Line:HCT116 human colon adenocarcinoma cells
-
Concentration:3 μM
-
Incubation Time:24 h
-
Result:Reduced cyclin A2 and CDK2 mRNA expression, whereas cyclin B1 and CDK1 mRNA expression were not affected.
-
Cell Line:HCT116 and Caco-2 colorectal cancer cells
-
Concentration:3 μM
-
Incubation Time:24 h
-
Result:Reduced migration of HCT116 and Caco-2 colorectal cancer cells in a PPAR-α/TRPV1-independent manner.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c nude (female, 6-8 weeks old, injected HCT116 cells (2.5 x 106, 200 μl PBS)[3]
-
Dosage:20 mg/kg
-
Administration:peritumoural; three times per week (every 2 days); 15 days
-
Result:Reduced xenograft tumour volume compared with vehicle over 7 measurements after first administration.
Excised tumours were smaller and had lower weights.
Ki-67-positive cells and Ki-67 red intensity mean value were reduced in tumours.
Tumour OEA levels were increased, whereas PEA and anandamide levels were not altered.
Did not alter tumour PPAR-α, TRPV1, or CB receptor gene expression, and exploratory data showed no alteration of pAKT, ERK1/2, or pS6.
Tumour secretomes from mice showed reduced levels of EGF-family members Erb-B1, Erb-B2, Erb-B3, and AREG.
-
Animal Model:CD1 (male, 6 weeks old, Azoxymethane at the single dose of 10 mg/kg, once per week for 4 weeks)[3]
-
Dosage:20 mg/kg
-
Administration:i.p.; three times per week (every 2 days); 13 weeks, starting 1 week before first Azoxymethane administration
-
Result:Reduced the number of azoxymethane-induced tumours by approximately 40%.
- RT-PCR
- Collagen: Sirius Red Staining
- RNA extraction experimental
- Cell migration
- BrdU Incorporation Assay
- Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- Protocol for Cell Cycle
- Real Time qPCR (Q-PCR)
- Cell Viability Determination by MTT Colorimetric Assay
- Phagocytosis Functional Assay
- Fibrosis/Collagen Morphometry
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Flow cytometric DNA-content cell-cycle staining
- DSS-Induced Colitis
- TNBS-Induced Colitis
- Patient-Derived Xenograft (PDX)
- Primary monocyte-to-macrophage differentiation
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
-
CAS No. 157469-21-1
-
Appearance Liquid (Density: 0.94±0.1 g/cm3)
-
Molecular Weight 275.45
-
Formula C17H25NS
-
Color Light yellow to yellow
-
SMILES
S=C=NCCCCCCCCCCC1=CC=CC=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (181.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 5 mg/mL (18.15 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (282 KB)
-
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
-
Handling Instructions (2659 KB)
References
[2]. Nanì MF, et al. Pharmacological Inhibition of N-Acylethanolamine Acid Amidase (NAAA) Mitigates Intestinal Fibrosis Through Modulation of Macrophage Activity. Journal of Crohn's & colitis. 2025 Feb 04;19(2):jjae132. [Content Brief]
[3]. Romano B, et al. N-Acylethanolamine acid amidase (NAAA) is dysregulated in colorectal cancer patients and its inhibition reduces experimental cancer growth. British journal of pharmacology. 2022 Apr;179(8):1679-1694. [Content Brief]
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.6304 mL | 18.1521 mL | 36.3042 mL | 90.7606 mL |
| 5 mM | 0.7261 mL | 3.6304 mL | 7.2608 mL | 18.1521 mL | |
| 10 mM | 0.3630 mL | 1.8152 mL | 3.6304 mL | 9.0761 mL | |
| 15 mM | 0.2420 mL | 1.2101 mL | 2.4203 mL | 6.0507 mL | |
| 20 mM | 0.1815 mL | 0.9076 mL | 1.8152 mL | 4.5380 mL | |
| 25 mM | 0.1452 mL | 0.7261 mL | 1.4522 mL | 3.6304 mL | |
| 30 mM | 0.1210 mL | 0.6051 mL | 1.2101 mL | 3.0254 mL | |
| 40 mM | 0.0908 mL | 0.4538 mL | 0.9076 mL | 2.2690 mL | |
| 50 mM | 0.0726 mL | 0.3630 mL | 0.7261 mL | 1.8152 mL | |
| 60 mM | 0.0605 mL | 0.3025 mL | 0.6051 mL | 1.5127 mL | |
| 80 mM | 0.0454 mL | 0.2269 mL | 0.4538 mL | 1.1345 mL | |
| 100 mM | 0.0363 mL | 0.1815 mL | 0.3630 mL | 0.9076 mL |
AM9053 Related Classifications
HY-185011 Related Classifications
Powered by Bioz