SCH58261

製品コードS8104 バッチS810403

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₈H₁₅N₇O

分子量

345.36

CAS No.

160098-96-4

Solubility (25°C)*

体外

DMSO

35 mg/mL (101.34 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

4%DMSO 1 40%PEG300 2 4%Tween80 3 52%ddH2O

2.0mg/ml

Taking the 1 mL working solution as an example, add 40 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 40 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 520 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	SCH 58261 is a potent and selective A2a adenosine receptor antagonist with K_i of 2.3 nM and 2 nM for rat A2a and bovine A2a, respectively.
in vitro	SCH 58261 causes the inhibition of rabbit platelet aggregation and porcine coronary artery relaxation by antagonizing competitively the effects induced by CGS 21680. ^[1]
in vivo	In mice with Spinal cord injury, SCH58261 (0.01 mg/kg, i.p.) reduces demyelination and levels of TNF-α, Fas-L, PAR, Bax expression and activation of JNK MAPK. Chronic SCH58261 administration improves the neurological deficit up. ^[2] In rats with 6-OHDA-induced Parkinson's disease, SCH58261 (2 mg/kg, i.p.) improves the 6-OHDA-induced bradykinesia and motor disturbance. ^[3]

製品説明

SCH 58261 is a potent and selective A2a adenosine receptor antagonist with K_i of 2.3 nM and 2 nM for rat A2a and bovine A2a, respectively.

in vitro

SCH 58261 causes the inhibition of rabbit platelet aggregation and porcine coronary artery relaxation by antagonizing competitively the effects induced by CGS 21680. ^[1]

in vivo

In mice with Spinal cord injury, SCH58261 (0.01 mg/kg, i.p.) reduces demyelination and levels of TNF-α, Fas-L, PAR, Bax expression and activation of JNK MAPK. Chronic SCH58261 administration improves the neurological deficit up. ^[2]

In rats with 6-OHDA-induced Parkinson's disease, SCH58261 (2 mg/kg, i.p.) improves the 6-OHDA-induced bradykinesia and motor disturbance. ^[3]

プロトコル(参考用のみ)

キナーゼアッセイ	Receptor binding assay
キナーゼアッセイ	Rat brain tissues (cortex and striatum) are obtained from male Sprague-Dawley rats weighing 250 to 300 g. Bovine brain tissues (frontal cortex and striatum) are obtained from a local abattoir within 10 mm from animal sacrifice. A1 and A2a ADO receptor binding assays are performed using [³H]CHA and [³H]CGS 21680 [³H]2-[4-(2-carboxyethyl)-phenethylamino]- 5’-N-ethylcarboxamidoadenosinel as radioligands, respectively. Binding assay to CHO cells stably transfected with the rat brain A3 ADO receptor is performed using [¹²⁵I]AB-MECA as radioligand. In order to determine the type of inhibition (competitive or noncompetitive), saturation experiments at A1 ADO ([³H]CHA, 0.125-64 nM) and A2a ADO receptors ([³HJCGS 21680, 1-128 aM) are carried out on rat brain tissues in the absence or in the presence of different concentrations of SCH 58261 (7-(2-phenylethyl)-5-amino-2-(2-furyl)-pyrazolo-[4,3-e]-1,2,4- triazolo[1,5-c]pyrimidine}. The affinity of SCH 58261 for several neurotransmitter binding sites, such as alpha-1, alpha-2 and beta-1 adrenoceptors, D1 and D2 dopamine receptors, 5-HT1 and 5-HT2 receptors, M1 and M2 muscarinic receptors, mu-opioid, benzodiazepine and N-methyl-D-aspartate receptors, is measured according to standard methods.
細胞アッセイ	細胞株	Astrocytes
	濃度	200 nM
	反応時間
	実験の流れ	Cells were treated with indicated concentrations of drug.
動物実験	動物モデル	Mice with Spinal cord injury
	投薬量	0.01 mg/kg
	投与方法	i.p.

参考

[4] Hou X, et al. PPAR Res. 2020 Mar 6;2020:2410264.

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Adenosine A2A Receptor Antagonist Improves Cognitive Impairment by Inhibiting Neuroinflammation and Excitatory Neurotoxicity in Chronic Periodontitis Mice [ Molecules, 2022, 27(19)6267]	PubMed: 36234803
The adenosine A2A receptor alleviates postoperative delirium-like behaviors by restoring blood cerebrospinal barrier permeability in rats [ J Neurochem, 2021, 10.1111/jnc.15436]	PubMed: 34033116
Electroacupuncture improves neuronal plasticity through the A2AR/cAMP/PKA signaling pathway in SNL rats [ Neurochem Int, 2021, 145:104983]	PubMed: 33577869
Targeting of the A2A adenosine receptor counteracts immunosuppression in vivo in a mouse model of chronic lymphocytic leukemia. [ Haematologica, 2020, 16 pii: haematol]	PubMed: 32299906
Neuronal mechanisms of adenosine A 2A receptors in the loss of consciousness induced by propofol general anesthesia with functional magnetic resonance imaging (fMRI) [ J Neurochem, 2020, 10.1111/jnc.15146]	PubMed: 32785947
Adenosine Receptor A1-A2a Heteromers Regulate EAAT2 Expression and Glutamate Uptake via YY1-Induced Repression of PPARγ Transcription. [ PPAR Res, 2020, 2020:2410264]	PubMed: 32206061

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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