SCH 58261 |
Catalog No.GC14565
One-Click Copy Product Info
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SCH 58261 is a potent and selective non-xanthine A2A adenosine antagonist, with an IC50 of 15nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 160098-96-4
Sample solution is provided at 25 µL, 10mM.
SCH 58261 is a potent and selective non-xanthine A2A adenosine antagonist, with an IC50 of 15nM[1]. SCH 58261 has been widely used in animal models of cardiovascular and neurological regulation[2].
In vitro, SCH 58261 treatment (50nM; 24h) reduced microglia proliferation as well as the expression and release of pro-inflammatory mediators in rat retinal nerve cell culture[3].
In vivo, SCH 58261 treatment at a single dose of 5mg/kg (i.p.) for 90min reversed reserpine-induced muscle stiffness and attenuated reserpine-enhanced tonic and reflex electromyographic activity in gastrocnemius and tibial muscles[4]. Systemic administration of SCH 58261 (5mg/kg; i.p.; 3 times, every 3h, 10min before haloperidol) within one day partially decreased the haloperidol-induced catalepsy and the increase in the proenkephalin (PENK) expression in both dorsolateral and ventrolateral parts of the striatum of rats[5]. In rats, intraperitoneal injection of SCH 58261 at a single dose of 10mg/kg for one day enhanced exercise capacity, increased alertness, and slightly increased blood pressure and heart rate[6]. Intraperitoneal injection of SCH 58261 (0.01mg/kg) administered 5 minutes after middle cerebral artery occlusion (MCAO) inhibited turning behavior in rats and significantly reduced the outflow of glutamate, markedly decreasing cortical damage without preventing sensorimotor impairment[7].
References:
[1] Zocchi C, Ongini E, Conti A, et al. The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2a adenosine receptor antagonist[J]. The Journal of pharmacology and experimental therapeutics, 1996, 276(2): 398-404.
[2] Monopoli A, Casati C, Lozza G, et al. Cardiovascular pharmacology of the A2A adenosine receptor antagonist, SCH 58261, in the rat[J]. The Journal of pharmacology and experimental therapeutics, 1998, 285(1): 9-15.
[3] Aires I D, Boia R, Rodrigues‐Neves A C, et al. Blockade of microglial adenosine A2A receptor suppresses elevated pressure‐induced inflammation, oxidative stress, and cell death in retinal cells[J]. Glia, 2019, 67(5): 896-914.
[4] Wardas J, Konieczny J, Lorenc‐Koci E. SCH 58261, an A2A adenosine receptor antagonist, counteracts parkinsonian‐like muscle rigidity in rats[J]. Synapse, 2001, 41(2): 160-171.
[5] Wardas J, Pietraszek M, Dziedzicka-Wasylewska M. SCH 58261, a selective adenosine A2A receptor antagonist, decreases the haloperidol-enhanced proenkephalin mRNA expression in the rat striatum[J]. Brain research, 2003, 977(2): 270-277.
[6] Ongini E. SCH 58261: A selective A2A adenosine receptor antagonists[J]. Drug development research, 1997, 42(2): 63-70.
[7] Melani A, Pantoni L, Bordoni F, et al. The selective A2A receptor antagonist SCH 58261 reduces striatal transmitter outflow, turning behavior and ischemic brain damage induced by permanent focal ischemia in the rat[J]. Brain Research, 2003, 959(2): 243-250.
| Cell experiment [1]: | |
Cell lines | Rat primary retinal neural cell |
Preparation Method | Primary retinal neural cell cultures were prepared from 3 to 5-day-old Wistar rats. The cells were plated at a density of 2×106 cells/cm2 in 12‐well plates with glass coverslips, all precoated with poly‐d‐lysine (0.1mg/mL). Cells were cultured at 37°C in a humidified atmosphere of 5% CO2 for 7 days. Cell cultures were incubated with 50nM of the SCH 58261 for 45min before placing the cultures inside the pressure chamber. Cultures were submitted to elevated hydrostatic pressure (EHP; 70 mmHg above atmospheric pressure) for 24h. The morphology and proliferation ability of the cells were analyzed. |
Reaction Conditions | 50nM; 24h |
Applications | SCH 58261 treatment prevented cell morphological changes and reduced cell death caused by high pressure in rat primary retinal neural cells. |
| Animal experiment [2]: | |
Animal models | Wistar rats |
Preparation Method | Male Wistar rats weighing 270-290g were used and kept 3 rats per cage with free access to food and water. All rats were kept on a 12-h light/dark cycle (lights on at 8: 00 am) in standardized temperature, humidity and light conditions with free access to food and water. Focal cerebral ischemia was produced by a permanent middle cerebral artery occlusion (MCAO) in the right hemisphere. Rats were anesthetized with 5.0% isoflurane and spontaneously inhaled 1.0 to 2.0% isoflurane in air by use of a mask. Body core temperature was maintained at 37 °C with the recirculating pad and K module and monitored via an intrarectal type T thermocouple. The rats were placed in a stereotaxic frame and the surgical procedure to occlude MCAO consisted of the insertion of a 4-0 nylon monofilament, pre-coated with silicone mixed with a hardener, via the external carotid artery into the internal carotid artery to block the origin of MCAO. Sham-operated rats were used as control in which the filament was inserted into the internal carotid artery and then withdrawn. After the end of the surgical procedure anesthesia was discontinued, the rats were placed in a prone position, and were then allowed to recover from anesthesia. Recovery from anesthesia lasted for about 15min, thereafter, rats had free access to food and water. SCH 58261 was dissolved by sonication in saline with 1% Tween 80. In SCH 58261-treated and vehicle-treated rats, the SCH 58261 or vehicle was administered intraperitoneally 5min at a dose of 0.01mg/kg once after occlusion. Rats were sacrificed after one day from the experiment and brain tissues were collected for histological analysis. |
Dosage form | 0.01mg/kg for once; i.p. |
Applications | SCH 58261 treatment significantly improved the neurological deficit and reduced ischemic damage in the striatum and cortex of rats. |
References: | |
| Cas No. | 160098-96-4 | SDF | |
| Chemical Name | 2-(furan-2-yl)-7-phenethyl-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine | ||
| Canonical SMILES | NC1=NC(N(CCC2=CC=CC=C2)N=C3)=C3C4=NC(C5=CC=CO5)=NN41 | ||
| Formula | C18H15N7O | M.Wt | 345.36 |
| Solubility | ≥ 34.5mg/mL in DMSO | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8955 mL | 14.4776 mL | 28.9553 mL |
| 5 mM | 579.1 μL | 2.8955 mL | 5.7911 mL |
| 10 mM | 289.6 μL | 1.4478 mL | 2.8955 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)