Referencia número: HY-19532

ZM241385

Name: ZM241385
Brand: MedChemExpress
SKU: HY-19532
Price: 66.00 USD
Availability: InStock
Rating: 5 (17 reviews)

17 Cited Publications

Revisión del cliente

Based on 17 publication(s) in Google Scholar

ZM241385 is a potent, high affinity and selective adenosine A_2a receptor (A_2AR) antagonist with a K_i value of 1.4 nM.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza : 99.34%
No. CAS: 139180-30-6
Fòrmula: C₁₆H₁₅N₇O₂
Peso molecular:337.34

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

ZM241385 Chemical Structure

No. CAS: 139180-30-6

Tamaño

Precio

Stock

Cantidad

Amount: USD 0.00

* Seleccione Cantidad antes de agregar artículos.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (17)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

ZM241385 is a potent, high affinity and selective adenosine A_2a receptor (A_2AR) antagonist with a K_i value of 1.4 nM^[1]^[2]^[3].

IC₅₀ & Target

^[2] ^[1]

A2AR

1.4 nM (Ki)

Ver todos los productos específicos de isoformas Adenosine Receptor :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	42 nM Compound: 5, ZM 241385	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	[PMID: 23602401]
CHO	IC₅₀	33 nM Compound: 1, ZM 241385	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	[PMID: 25490054]
CHO	EC₅₀	>100000 nM Compound: 1, ZM 241385	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	[PMID: 25490054]
CHO	IC₅₀	0.678 nM Compound: 1; ZM 241385	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	[PMID: 27933962]
CHO	IC₅₀	1.45 nM Compound: 1; ZM 241385	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	[PMID: 27933962]
CHO	IC₅₀	48 nM Compound: 1; ZM 241385	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	[PMID: 27933962]

In Vitro

ZM241385 (1 μM; 24-48 hours; PC12 cells) treatment reverses the phenomenon that A_2AR agonist CGS21680 significantly upregulates A_2AR mRNA and protein levels^[1].

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

RT-PCR^[1]

Cell Line:

PC12 cells
Concentration:

1 μM
Incubation Time:

24 hours
Result:

Suppressed the increased A_2AR mRNA levels engendered by CGS21680.

Western Blot Analysis^[1]

Cell Line:

PC12 cells
Concentration:

1 μM
Incubation Time:

48 hours
Result:

Decreased A_2AR protein levels

In Vivo

ZM241385 (0.2 μg/mouse, 0.4 μg/mouse; intraperitoneal injection; every day; for 11 weeks; female C57BL/6 WT mice) treatment decreases tumor volume, activates CD8⁺ T cells and reduces the frequency of splenic MDSC^[4].

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

Animal Model:

Female C57BL/6 WT mice received 4-nitroquinoline-N-oxide^[4]
Dosage:

0.2 μg/mouse, 0.4 μg/mouse
Administration:

Intraperitoneal injection; every day; for 11 weeks
Result:

Decreased tumor volume, activates CD8⁺ T cells and reduces the frequency of splenic MDSC.

Chemical Information

No. CAS 139180-30-6
Appearance Solid
Peso molecular 337.34
Fòrmula C₁₆H₁₅N₇O₂
Color White to off-white
SMILES

OC1=CC=C(CCNC2=NC3=NC(C4=CC=CO4)=NN3C(N)=N2)C=C1
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (17)

All Bio/Physico-chemical AssayELISAIn Vivo Efficacy StudyFlow CytometryWB

Sort by:

Journal Impact Factor

Mater Today

2024 Apr 26.

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.
Nat Neurosci

Lipid-accumulated reactive astrocytes promote disease progression in epilepsy. [Abstract]

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.
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.
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 May;12(20):e2409837. PMID: 40289872
Cell Death Differ

2026 Aug 18. PMID: 42613426
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
Cell Mol Gastroenterol Hepatol

Extracellular Inosine Induces Anergy in B Cells to Alleviate Autoimmune Hepatitis. [Abstract]

2025;19(10):101539. PMID: 40409684
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 A_2aR, in A549 cells.
Biochem Pharmacol

Exosomal CD73 from endometrial regenerative cells confers protective effects against ischemia-reperfusion injury in kidney transplantation. [Abstract]

2026 Sep;251(Pt 1):118080. PMID: 42162765
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
Authorea

2025 Oct 7.
SSRN

2022.

Solvente y solubilidad

In Vitro:

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)

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

2.9644 mL

14.8218 mL

29.6437 mL

5 mM

0.5929 mL

2.9644 mL

5.9287 mL

10 mM

0.2964 mL

1.4822 mL

2.9644 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, 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

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: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 6.25 mg/mL (18.53 mM); Clear solution

Protocol 2

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.

Protocol 3

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.

Protocol 4

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

Solubility: ≥ 5 mg/mL (14.82 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 12.5 mg/mL (37.05 mM); Clear solution; Need ultrasonic

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (277 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 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)
Instrucciones de manejo (2659 KB)

Referencias

[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]

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

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

Bioz

Keywords

ZM241385

17 Cited Publications

100 mg Obtener un presupuesto

Subscribe to the

MedChemExpress

Newsletter

Nombre del producto:
Referencia número:
Cantidad:
MCE Japan Authorized Agent:

Nombre del producto:
No. CAS:
Species:
Pureza:
Cantidad:

ZM241385

Publications Citing Use of MedChemExpress (MCE) ZM241385

Ver todos los productos específicos de isoformas Adenosine Receptor