ZM 241385
Catalog No.: GC11017Purity:>99.00%
ZM 241385 is a potent, high-affinity, and selective adenosine A2A receptor (A2AR) antagonist with a Ki value of 0.4±0.03nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 139180-30-6
10mM (in 1mL DMSO)In Stock
$46.00
1
5mgIn Stock
$42.00
1
10mgIn Stock
$67.00
1
25mgIn Stock
$132.00
1
50mgIn Stock
$211.00
1
100mgIn Stock
$317.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $46.00 | In Stock | 1 | |
| 5mg | $42.00 | In Stock | 1 | |
| 10mg | $67.00 | In Stock | 1 | |
| 25mg | $132.00 | In Stock | 1 | |
| 50mg | $211.00 | In Stock | 1 | |
| 100mg | $317.00 | In Stock | 1 |
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com
Citations
1 publicationsPublications from researchers using this productDescription
ZM 241385 is a potent, high-affinity, and selective adenosine A2A receptor (A2AR) antagonist with a Ki value of 0.4±0.03nM[1]. By regulating A2AR, ZM 241385 attenuated the vasodilation response caused by exogenous adenosine in the hindlimbs after constant-flow perfusion and reduced the increase in arterial blood pressure caused by exogenous adenosine[2]. ZM 241385 has been widely used in preclinical models to regulate the functions of the central nervous system and has been employed as a reference compound for the development of A2A receptor antagonists[3].
In vitro, ZM 241385 treatment (10nM) for 10 minutes reduced Src kinase phosphorylation, β-arrestin recruitment, and ERK phosphorylation induced by D2 receptors in HEK293 cells[4]. Treatment with 100nM ZM 241385 for 7 minutes increased the neuronal survival rate of rat CA1 hippocampal slices under hypoxic and hypoglycemic conditions and reduced the expression of the 30kDa fragment of GFAP[5]. 1µM of ZM 241385 pretreatment for 30 minutes reversed the p44/42 MAPK phosphorylation elicited by CGS21680 in PC12 cells and decreased the nitrite level[6]. 100nM of ZM 241385 pretreatment for 30 minutes inhibited CGS21680-induced proliferation of MRMT-1, A375, and A549 cells[7].
In vivo, a single intraperitoneal injection of ZM 241385 at a dose of 1mg/kg at 30 minutes before the induction of hyperglycemic cerebral ischemia alleviated hippocampal injury and neurobehavioral deficits in rats[8]. A single intravitreal injection of ZM 241385 (50µM; 1µl) at 2 weeks later mitigated microglial morphological changes and inflammatory responses in the retina of rats with chronic ocular hypertension[9].
References:[1] Guo D, Xia L, van Veldhoven J P D, et al. Binding kinetics of ZM241385 derivatives at the human adenosine A2A receptor[J]. ChemMedChem, 2014, 9(4): 752-761.
[2] Keddie J R, Poucher S M, Shaw G R, et al. In vivo characterisation of ZM 241385, a selective adenosine A2A receptor antagonist[J]. European journal of pharmacology, 1996, 301(1-3): 107-113.
[3] Byeon J J, Park M H, Shin S H, et al. In vitro, in silico, and in vivo assessments of pharmacokinetic properties of Zm241385[J]. Molecules, 2020, 25(5): 1106.
[4] Huang L, Wu D, Zhang L, et al. Modulation of A2a receptor antagonist on D2 receptor internalization and ERK phosphorylation[J]. Acta Pharmacologica Sinica, 2013, 34(10): 1292-1300.
[5] Pugliese A M, Traini C, Cipriani S, et al. The adenosine A2A receptor antagonist ZM241385 enhances neuronal survival after oxygen‐glucose deprivation in rat CA1 hippocampal slices[J]. British journal of pharmacology, 2009, 157(5): 818-830.
[6] Wang Z, Che P L, Du J, et al. Static magnetic field exposure reproduces cellular effects of the Parkinson's disease drug candidate ZM241385[J]. PLoS One, 2010, 5(11): e13883.
[7] Gessi S, Bencivenni S, Battistello E, et al. Inhibition of A2A adenosine receptor signaling in cancer cells proliferation by the novel antagonist TP455[J]. Frontiers in pharmacology, 2017, 8: 888.
[8] Higashi H, Meno J R, Marwaha A S, et al. Hippocampal injury and neurobehavioral deficits following hyperglycemic cerebral ischemia: effect of theophylline and ZM 241385[J]. Journal of neurosurgery, 2002, 96(1): 117-126.
[9] Liu X, Huang P, Wang J, et al. The effect of A2A receptor antagonist on microglial activation in experimental glaucoma[J]. Investigative ophthalmology & visual science, 2016, 57(3): 776-786.
Protocol
| Cell experiment [1]: | |
|
Cell lines |
A375 cells |
|
Preparation Method |
A375 cells were cultured in DMEM medium, supplemented with 10% fetal bovine serum and 1% penicillin-streptomycin, at 37°C in an incubator with 5% CO2. Cells were cultured over night at 1000 cells/well in a 96-well plate, and cells were pretreated for 30min with 100nM ZM 241385 before stimulation with 100nM CGS21680 for 48h, the cell proliferation was measured. |
|
Reaction Conditions |
100nM; 30min |
|
Applications |
ZM 241385 treatment markedly inhibited CGS21680-induced cell proliferation in A375 cells. |
| Animal experiment [2]: | |
|
Animal models |
Male Wistar rats |
|
Preparation Method |
Male Wistar rats (300-400g) were kept at room temperature (25 ± 2°C), with a light-dark cycle of 12h and a humidity of 60±10%. Thirty minutes before the onset of ischemia, rats received intraperitoneal injections of theophylline (36mg/kg), ZM 241385 (1mg/kg), or an equivalent volume of saline. The hyperglycemic groups were given an intraperitoneal injection of 17% D-glucose (3g/kg) 15 minutes before ischemia was induced. The normoglycemic groups received an equivalent volume of saline intraperitoneally. Morris water maze trials were performed on the 7th day after ischemic insult. After the conclusion of the performance tests, the rat brains were cut into 8-xm sections, stained with cresyl violet and acid fuchsin, and evaluated in a blinded fashion to determine the extent of injury. |
|
Dosage form |
1mg/kg; once; i.p. |
|
Applications |
ZM 241385 treatment mitigated hippocampal injury and neurobehavioral deficits in rats following hyperglycemic cerebral ischemia. |
| References: [1] Gessi S, Bencivenni S, Battistello E, et al. Inhibition of A2A adenosine receptor signaling in cancer cells proliferation by the novel antagonist TP455[J]. Frontiers in pharmacology, 2017, 8: 888. [2] Higashi H, Meno J R, Marwaha A S, et al. Hippocampal injury and neurobehavioral deficits following hyperglycemic cerebral ischemia: effect of theophylline and ZM 241385[J]. Journal of neurosurgery, 2002, 96(1): 117-126. | |
Product Documents
Purity:>99.00%Appearance:A solid
Chemical Properties
CAS No.
139180-30-6
Chemical Name
4-(2-((7-amino-2-(furan-2-yl)-[1,2,4]triazolo[1,5-a][1,3,5]triazin-5-yl)amino)ethyl)phenol
SMILES
OC1=CC=C(C=C1)CCNC2=NC3=NC(C4=CC=CO4)=NN3C(N)=N2
Molecular Formula
C16H15N7O2
Molecular Weight
337.34
Solubility
DMSO: 100mM,Ethanol: 5 mM
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
Reviews
Review for ZM 241385
Rating: 5
- 5 Star100%
- 4 Star0%
- 3 Star0%
- 2 Star0%
- 1 Star0%