ZM241385

Catalog No.S8105 Batch:S810501

Technical Data

Formula	C₁₆H₁₅N₇O₂
Molecular Weight	337.34	CAS No.	139180-30-6
Solubility (25°C)*	In vitro	DMSO	67 mg/mL (198.61 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

ZM-241385 is a high affinity antagonist ligand selective for the adenosine A2A receptor.

Targets

adenosine A2A receptor ^[3]

In vitro

ZM 241385 has high affinity for A2a receptors. In rat phaeochromocytoma cell membranes, ZM 241385 displaces binding of tritiated 5'-N-ethylcarboxamidoadenosine (NECA) with a pIC50 of 9.52^[3]. ZM241385 delays the appearance of anoxic depolarization (AD), a phenomenon strictly related to cell damage and death, protect from the synaptic activity depression brought about by a severe (7 min) OGD period, and protect CA1 neuron and astrocyte from injury^[4].

In vivo

ZM-241385 significantly blunts the hypotensive effects of CCPA and NECA without altering the bradycardia induced by these agonists. It blocks the infarct size-reducing effects(cardioprotective effects) of this two distinct adenosine receptor agonists^[1].

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines PC12 cells Concentrations 1 μM Incubation Time 24 h Method Nitric oxide (NO) production is assessed by measuring the amount of nitrite, a stable metabolic product of NO that provides an indirect measurement of NO, by using the Griess diazotization reaction. Briefly, 24 h after incubation with 1.0 µM CG21680 or 1.0 µM ZM241385 or exposure to SMF, samples of medium (150 µl) are collected from cells and mixed with 130 µl dH2O and with 20 µl Griess reagent using instruction supplied by the manufacturer. After a 30 min incubation period at room temperature, the samples are evaluated spectrophotometrically at 548 nm and OD values-in comparison with a standard curve is determined in culture medium by using serial dilutions of sodium nitrite-represented total stable metabolites of NO.
Animal Study:^{^[1]}	Animal Models Adult Sprague-Dawley rats Dosages 1.5 mg/kg Administration i.v.

Cell Assay:^{^[2]}

Cell lines
PC12 cells
Concentrations
1 μM
Incubation Time
24 h
Method
Nitric oxide (NO) production is assessed by measuring the amount of nitrite, a stable metabolic product of NO that provides an indirect measurement of NO, by using the Griess diazotization reaction. Briefly, 24 h after incubation with 1.0 µM CG21680 or 1.0 µM ZM241385 or exposure to SMF, samples of medium (150 µl) are collected from cells and mixed with 130 µl dH2O and with 20 µl Griess reagent using instruction supplied by the manufacturer. After a 30 min incubation period at room temperature, the samples are evaluated spectrophotometrically at 548 nm and OD values-in comparison with a standard curve is determined in culture medium by using serial dilutions of sodium nitrite-represented total stable metabolites of NO.

Animal Study:^{^[1]}

Animal Models
Adult Sprague-Dawley rats
Dosages
1.5 mg/kg
Administration
i.v.

References

[4] Pedata F, et al. Mediators Inflamm. 2014: 805198.

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Customer Product Validation

: Data from [Data independently produced by , , Biochem Pharmacol, 2018, doi: 10.1016/j.bcp.2018.01.033]

Selleck's ZM241385 has been cited by 7 publications

Adenosine Kinase Inhibition Prevents Severe Acute Pancreatitis via Suppressing Inflammation and Acinar Cell Necroptosis [ Front Cell Dev Biol, 2022, 10:827714]	PubMed: 35281076
Exogenous adenosine activates A2A adenosine receptor to inhibit RANKL-induced osteoclastogenesis via AP-1 pathway to facilitate bone repair [ Mol Biol Rep, 2021, 10.1007/s11033-021-07017-1]	PubMed: 34846650
Ticagrelor Inhibits the NLRP3 Inflammasome to Protect Against Inflammatory Disease Independent of the P2Y 12 Signaling Pathway [ Cell Mol Immunol, 2020, 10]	PubMed: 32523112
Blockade of Adenosine A 2A Receptor Protects Photoreceptors after Retinal Detachment by Inhibiting Inflammation and Oxidative Stress [ Oxid Med Cell Longev, 2020, 2020:7649080]	PubMed: 32714489
The Adenosine A2A Receptor Agonist Accelerates Bone Healing and Adjusts Treg/Th17 Cell Balance Through Interleukin 6 [ Biomed Res Int, 2020, 2020:2603873]	PubMed: 32382539
The cAMP-Adenosine Feedback Loop Maintains the Suppressive Function of Regulatory T Cells [ J Immunol, 2019, 203(6):1436-1446]	PubMed: 31420466
A novel combination of astilbin and low-dose methotrexate respectively targeting A2AAR and its ligand adenosine for the treatment of collagen-induced arthritis [Ma Y Biochem Pharmacol, 2018, 153:269-281]	PubMed: 29410374

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.