AR-C118925XX
Based on 4 publication(s) in Google Scholar
AR-C118925XX is a selective P2Y2 receptor antagonist. AR-C118925XX inhibits ATP-induced IL-6 production and phosphorylation of p38. AR-C118925XX also inhibits Bleomycin (HY-108345)-induced dermal fibrosis in mice. AR-C118925XX also inhibits ATP-induced tumor growth.
For research use only. We do not sell to patients.
- Purity : 98.02%
- CAS No.: 216657-60-2
- Formula: C28H23N7O3S
- Molecular Weight:537.59
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Storage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) AR-C118925XX
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Customer Validation & Images
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IF
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Cell Migration/Invasion Assay
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Bio/Physico-chemical Assay
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Cell Migration/Invasion Assay
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IF
All P2Y Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
P2Y2 Receptor |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 216657-60-2
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Appearance Solid
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Molecular Weight 537.59
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Formula C28H23N7O3S
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Color Light yellow to yellow
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SMILES
O=C(C1=CC=C(CN2C=C(C3C4=CC=C(C)C=C4C=CC5=CC(C)=CC=C53)C(NC2=O)=S)O1)NC6=NN=NN6
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (4)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Chemotherapy triggers immune evasion by fostering LEPR+ Kupffer cell differentiation in liver metastases. [Abstract]2026 Mar 9;44(3):658-675.e12. PMID: 41687606
AR-C118925XX purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2026 Mar 9;44(3):658-675.e12. [Abstract]
Representative immunofluorescence images and quantification of LEPR+DAB2+ KCs in mouse LMs (n = 10 mice/group). Scale bars, 100 μm. AR-C118925XX (10 mg/kg; i.p.; every 2 days, beginning 2 days after chemotherapy) reduced LEPR+ KCs infiltration into metastatic lesions.
AR-C118925XX purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2026 Mar 9;44(3):658-675.e12. [Abstract]
Schematic of the transwell assay to assess LEPR+ KCs chemotaxis towards 5-FU-treated AKP cells. Percentage of LEPR+ KCs migrating from the chamber treated with AR-C118925XX (10 μmol/L; 12 h).
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Am J Physiol Cell Physiol
2023 Nov 1;325(5):C1228-C1243. PMID: 37721000
AR-C118925XX purchased from MedChemExpress. Usage Cited in: Am J Physiol Cell Physiol. 2023 Nov 1;325(5):C1228-C1243. [Abstract]
Representative transmigration images and quantitative analysis of cells treated with P2Y2 blocker AR-C118925XX (100 nM; 18 h) (n = 20, scale bar = 100 µm). AR-C118925XX inhibited ATP-induced migration of CD34+ VW-SCs.
AR-C118925XX purchased from MedChemExpress. Usage Cited in: Am J Physiol Cell Physiol. 2023 Nov 1;325(5):C1228-C1243. [Abstract]
Representative images showing the migration and differentiation of CD34+ cells indicated by tdTomato (tdT) in matrigel plugs (scale bar = 50 μm). AR-C118925XX (100 nM; s.c.; single dose) inhibited ATP-driven CD34+ cell accumulation in Matrigel plugs and the increase in CD31+ cells colocalized with migrated CD34+ cells.
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AR-C118925XX purchased from MedChemExpress. Usage Cited in: Res Sq. 2025 May 18.
AR-C118925XX (100 μM; 24 h) reduced H2O2 levels in primary astrocytes with reactivity induced by H2O2.
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (186.02 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 (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.
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.
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: 2.5 mg/mL (4.65 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Protocols
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Fibrosis/Collagen Morphometry
Fibrosis and collagen morphometry is based on the quantitative visualization of fibrillar collagen deposition in tissue sections using histochemical stains such as Sirius Red (Picrosirius Red) or Masson's trichrome, followed by image-based or polarization-enhanced analysis to estimate collagen proportional area as a surrogate of extracellular matrix accumulation during fibrotic remodeling. Sirius Red combined with polarized light microscopy enhances detection of collagen fibers due to birefringence properties, enabling more specific visualization of collagen type I and III fibrils compared to conventional bright-field histology, while whole-section or region-restricted digital morphometry reduces field-selection bias in fibrosis assessment. Alternative quantitative approaches include second harmonic generation (SHG) and two-photon excited fluorescence microscopy, which enable label-free detection of fibrillar collagen and have been validated against histological staining and biochemica
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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Collagen: Sirius Red Staining
Sirius Red or picrosirius red staining is a histochemical method for visualizing collagen-rich extracellular matrix in tissue sections, and collagen fibers are detected as red-stained structures under bright-field microscopy with enhanced birefringence under polarized light. Picrosirius red is useful for assessing total collagen organization, distribution, and fibrosis burden, but polarized color should not be interpreted as a definitive collagen type I versus type III readout because color is affected by fiber orientation, thickness, and packing.
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Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
Masson’s Trichrome (collagen/trichrome staining) is a histological technique that differentially stains tissue compartments using sequential acidic dyes to distinguish collagen from muscle and cytoplasmic components based on dye affinity and tissue permeability differences, enabling visualization of fibrosis and connective tissue architecture in histological sections. The classical formulation typically uses Weigert's iron hematoxylin for nuclear staining, Biebrich scarlet-acid fuchsin for cytoplasm and muscle, and aniline blue (or light green variants) for collagen, producing a characteristic blue/green collagen signal contrasted against red cytoplasm and dark nuclei. The staining principle relies on selective displacement of smaller dye molecules by larger anionic dyes in collagen-rich regions under controlled acidified conditions, which enhances collagen-specific dye retention. This property makes the method widely used for fibrosis assessment in organs such as heart, liver, lung, a
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Patient-Derived Orthotopic Xenograft (PDOX)
Patient-derived orthotopic xenograft (PDOX) modeling implants fresh patient tumor tissue or patient-derived tumor cells into the anatomically corresponding organ or tissue site of immunodeficient mice, usually by surgical orthotopic implantation, to preserve patient tumor histology, local microenvironmental context, invasion, metastatic behavior, and treatment-response features better than subcutaneous implantation. PDOX readouts include tumor engraftment, orthotopic tumor growth, local invasion, metastasis, recurrence after resection, histologic similarity to the donor tumor, biomarker retention, molecular concordance, survival, and response or resistance to therapy. PDOX models are used for preclinical drug testing and individualized therapy evaluation, but engraftment success varies by tumor type and specimen quality.
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
Purity & Documentation
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Data Sheet (277 KB)
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SDS (544 KB)
- English - EN (544 KB)
- Français - FR (544 KB)
- Deutsch - DE (544 KB)
- Norwegian - NO (544 KB)
- Español - ES (544 KB)
- Swedish - SV (544 KB)
- Italian - IT (544 KB)
- Korean - KR (544 KB)
- Portuguese - PT (544 KB)
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Handling Instructions (2659 KB)
References
[1]. Perera LMB, et al. The Regulation of Skin Fibrosis in Systemic Sclerosis by Extracellular ATP via P2Y2 Purinergic Receptor. J Invest Dermatol. 2019 Apr;139(4):890-899. [Content Brief]
[2]. Dong CR, et al. AKT/GSK-3beta/VEGF signaling is involved in P2RY2 activation-induced the proliferation and metastasis of gastric cancer. Carcinogenesis. 2022 Dec 5:bgac095. [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 (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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.8602 mL | 9.3008 mL | 18.6015 mL | 46.5038 mL |
| 5 mM | 0.3720 mL | 1.8602 mL | 3.7203 mL | 9.3008 mL | |
| 10 mM | 0.1860 mL | 0.9301 mL | 1.8602 mL | 4.6504 mL | |
| 15 mM | 0.1240 mL | 0.6201 mL | 1.2401 mL | 3.1003 mL | |
| 20 mM | 0.0930 mL | 0.4650 mL | 0.9301 mL | 2.3252 mL | |
| 25 mM | 0.0744 mL | 0.3720 mL | 0.7441 mL | 1.8602 mL | |
| 30 mM | 0.0620 mL | 0.3100 mL | 0.6201 mL | 1.5501 mL | |
| 40 mM | 0.0465 mL | 0.2325 mL | 0.4650 mL | 1.1626 mL | |
| 50 mM | 0.0372 mL | 0.1860 mL | 0.3720 mL | 0.9301 mL | |
| 60 mM | 0.0310 mL | 0.1550 mL | 0.3100 mL | 0.7751 mL | |
| 80 mM | 0.0233 mL | 0.1163 mL | 0.2325 mL | 0.5813 mL | |
| 100 mM | 0.0186 mL | 0.0930 mL | 0.1860 mL | 0.4650 mL |
AR-C118925XX Related Classifications
HY-110126 Related Classifications
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