ZM241385
Based on 15 publication(s) in Google Scholar
ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM.
For research use only. We do not sell to patients.
- Purity: 99.45%
- CAS No.: 139180-30-6
- Formula: C16H15N7O2
- Molecular Weight:337.34
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ZM241385
More- Mater Today. 2024 Apr 26.
- Nat Neurosci. 2023 Apr;26(4):542-554. [Abstract]
- ACS Nano. 2025 Oct 21;19(41):36353-36372. [Abstract]
- ACS Nano. 2025 Mar 4;19(8):7962-7980. [Abstract]
- Adv Sci (Weinh). 2025 Apr 28:e2409837. [Abstract]
- Cell Mol Gastroenterol Hepatol. 2025 May 21:101539. [Abstract]
- Cell Chem Biol. 2025 Sep 18;32(9):1140-1149.e3. [Abstract]
- Mol Med. 2025 May 14;31(1):188. [Abstract]
- Ecotoxicol Environ Saf. 2023 Jan 1:249:114410. [Abstract]
- J Mol Cell Cardiol. 2023 Jan:174:88-100. [Abstract]
- Metab Brain Dis. 2026 May 28;41(1):119. [Abstract]
- Purinergic Signal. 2022 Sep;18(3):317-343. [Abstract]
- Int Urogynecol J. 2025 Apr;36(4):829-837. [Abstract]
- Authorea. 2025 Oct 7.
- SSRN. 2022.
Customer Validation & Images
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ELISA
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Flow Cytometry
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
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Flow Cytometry
All Adenosine Receptor Isoforms
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Biological Activity
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A2AR 1.4 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
42 nM
Compound: 5, ZM 241385
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Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
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[PMID: 23602401] |
| CHO | IC50 |
33 nM
Compound: 1, ZM 241385
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Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
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[PMID: 25490054] |
| CHO | EC50 |
>100000 nM
Compound: 1, ZM 241385
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Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
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[PMID: 25490054] |
| CHO | IC50 |
0.678 nM
Compound: 1; ZM 241385
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Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
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[PMID: 27933962] |
| CHO | IC50 |
1.45 nM
Compound: 1; ZM 241385
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Inverse agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
Inverse agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
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[PMID: 27933962] |
| CHO | IC50 |
48 nM
Compound: 1; ZM 241385
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Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
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[PMID: 27933962] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C57BL/6 WT mice received 4-nitroquinoline-N-oxide[4]
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Dosage:0.2 μg/mouse, 0.4 μg/mouse
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Administration:Intraperitoneal injection; every day; for 11 weeks
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Result:Decreased tumor volume, activates CD8+ T cells and reduces the frequency of splenic MDSC.
Chemical Information
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CAS No. 139180-30-6
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Appearance Solid
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Molecular Weight 337.34
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Formula C16H15N7O2
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Color White to off-white
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SMILES
OC1=CC=C(CCNC2=NC3=NC(C4=CC=CO4)=NN3C(N)=N2)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (15)
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Journal Impact Factor
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Most Recent
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ZM241385 purchased from MedChemExpress. Usage Cited in: Mater Today. 2024 Apr 26.
Bath application of ZM241385 (1 μM, 10 min) significantly inhibited seizure-like discharges in the brain slices of TLE participants.
ZM241385 purchased from MedChemExpress. Usage Cited in: Mater Today. 2024 Apr 26.
In vivo EEG recording of epileptic mice treated with vehicle or ZM241385 (2 mg/kg; i.p.; every other day for 3 weeks). The number of seizures per day and seizure duration were analyzed. The A2AR antagonist ZM241385 markedly reduced KA-induced seizure activities in mice.
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Nat Neurosci
2023 Apr;26(4):542-554. PMID: 36941428
ZM241385 purchased from MedChemExpress. Usage Cited in: Nat Neurosci. 2023 Apr;26(4):542-554. [Abstract]
Representative flow cytometric analysis, and quantitative of divided T cells after various treatments. ZM241385 reversed the inhibition effect of adenosine on T cells.
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ACS Nano
Surface d-Band Modulation via Biodirected Mineralization Enables Nanoenzymes to Inhibit Radiation-Induced T-Cell Exhaustion and Potentiate Immunoradiotherapy. [Abstract]2025 Oct 21;19(41):36353-36372. PMID: 41073355
ZM241385 purchased from MedChemExpress. Usage Cited in: ACS Nano. 2025 Oct 21;19(41):36353-36372. [Abstract]
Intracellular cAMP concentrations in CD8+ T cells after various treatments. Pretreatment with ZM241385 (10 μM; 12 h) can inhibit effects of SBRT by reducing cAMP levels.
ZM241385 purchased from MedChemExpress. Usage Cited in: ACS Nano. 2025 Oct 21;19(41):36353-36372. [Abstract]
Proportion of pCREB+CD8+ T cells after various treatments. Pretreatment with ZM241385 (10 μM; 12 h) can inhibit effects of SBRT by reducing CREB phosphorylation.
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ACS Nano
MnO2-Assisted Photosynthetic Bacteria Interfering with the Adenosine-A2AR Metabolic Pathway to Enhance Tumor Photothermal Immunotherapy. [Abstract]2025 Mar 4;19(8):7962-7980. PMID: 39976374 -
Adv Sci (Weinh)
Microbiota-Derived Inosine Suppresses Systemic Autoimmunity via Restriction of B Cell Differentiation and Migration. [Abstract]2025 Apr 28:e2409837. PMID: 40289872 -
Cell Mol Gastroenterol Hepatol
2025 May 21:101539. PMID: 40409684 -
Cell Chem Biol
Structural basis of adenosine 2A receptor-balanced signaling activation relies on allosterically mediated structural dynamics. [Abstract]2025 Sep 18;32(9):1140-1149.e3. PMID: 40925370 -
Mol Med
Arctiin, a lignan compound, enhances adipose tissue browning and energy expenditure by activating the adenosine A2A receptor. [Abstract]2025 May 14;31(1):188. PMID: 40369420 -
Ecotoxicol Environ Saf
A2aR inhibits fibrosis and the EMT process in silicosis by regulating Wnt/β-catenin pathway. [Abstract]2023 Jan 1:249:114410. PMID: 36516619
ZM241385 purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2023 Jan 1:249:114410. [Abstract]
ZM241385 (10 μM) significantly decreases the levels of E-cad, increases the N-cad, Vimentin, and α-SMA levels by inhibiting A2aR, in A549 cells.
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J Mol Cell Cardiol
Adenosine kinase promotes post-infarction cardiac repair by epigenetically maintaining reparative macrophage phenotype. [Abstract]2023 Jan:174:88-100. PMID: 36473288 -
Metab Brain Dis
TTP protects against 6-OHDA-induced dopaminergic neurodegeneration via astrocytic Nrf2/HO-1 activation in cellular and rat models of Parkinson's disease. [Abstract]2026 May 28;41(1):119. PMID: 42207326 -
Purinergic Signal
Lysophosphatidylcholine induces adenosine release from macrophages via TRPM7-mediated mitochondrial activation. [Abstract]2022 Sep;18(3):317-343. PMID: 35779163 -
Int Urogynecol J
A2A Adenosine Receptor as a Potential Therapeutic Target in Cystitis-Induced Bladder Pain: Insights from a Transgenic Autoimmune Cystitis Murine Model. [Abstract]2025 Apr;36(4):829-837. PMID: 39945803 -
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Solvent & Solubility
DMSO : 100 mg/mL (296.44 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (14.82 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (14.82 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 50% PEG300 50% Saline
Solubility: 12.5 mg/mL (37.05 mM); Clear solution; Need ultrasonic
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.
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
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Data Sheet (277 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
References
[1]. Wang Z, et al. Static magnetic field exposure reproduces cellular effects of the Parkinson's disease drugcandidate ZM241385. PLoS One. 2010 Nov 8;5(11):e13883. doi: 10.1371/journal.pone.0013883. [Content Brief]
[2]. Linden J, et al. Characterization of human A(2B) adenosine receptors: radioligandbinding, western blotting, and coupling to G(q) in human embryonickidney 293 cells and HMC-1 mast cells. Mol Pharmacol. 1999 Oct;56(4):705-13. [Content Brief]
[3]. Poucher SM, et al. The in vitro pharmacology of ZM 241385, a potent, non-xanthine A2a selective adenosinereceptor antagonist. Br J Pharmacol. 1995 Jul;115(6):1096-102. [Content Brief]
[4]. Ludwig S, et al. Impact of combination immunochemotherapies on progression of 4NQO-induced murine oral squamous cell carcinoma. Cancer Immunol Immunother. 2019 Jul;68(7):1133-1141. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9644 mL | 14.8218 mL | 29.6437 mL | 74.1092 mL |
| 5 mM | 0.5929 mL | 2.9644 mL | 5.9287 mL | 14.8218 mL | |
| 10 mM | 0.2964 mL | 1.4822 mL | 2.9644 mL | 7.4109 mL | |
| 15 mM | 0.1976 mL | 0.9881 mL | 1.9762 mL | 4.9406 mL | |
| 20 mM | 0.1482 mL | 0.7411 mL | 1.4822 mL | 3.7055 mL | |
| 25 mM | 0.1186 mL | 0.5929 mL | 1.1857 mL | 2.9644 mL | |
| 30 mM | 0.0988 mL | 0.4941 mL | 0.9881 mL | 2.4703 mL | |
| 40 mM | 0.0741 mL | 0.3705 mL | 0.7411 mL | 1.8527 mL | |
| 50 mM | 0.0593 mL | 0.2964 mL | 0.5929 mL | 1.4822 mL | |
| 60 mM | 0.0494 mL | 0.2470 mL | 0.4941 mL | 1.2352 mL | |
| 80 mM | 0.0371 mL | 0.1853 mL | 0.3705 mL | 0.9264 mL | |
| 100 mM | 0.0296 mL | 0.1482 mL | 0.2964 mL | 0.7411 mL |
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