CGS 21680 HCl

製品コードS2153 バッチS215301

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H29N7O6.HCl
分子量 535.98 CAS No. 124431-80-7
Solubility (25°C)* 体外 DMSO 107 mg/mL (199.63 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.

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生物活性

製品説明 CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor.
in vitro CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor. In an isolated perfused working rat heart model, CGS 21680C effectively increases coronary flow with an ED25 value of 1.8 nM. [1] CGS 21680 binds adenosine A2 receptor with high affinity (Kd = 15.5 nM) and limited capacity (apparent Bmax = 375 fmol/mg of protein) to a single dass of recognition sites.[2] In hippocampal slices, CGS 21680 apis weak agonist on pre- and postsynaptic measures of electrophysiologicaJ activity (putative Al receptor mediated events) and is ineffective at stimulating the formation of cAMP (a putative A2 mediated response). In striatal slices, CGS 21680 potently stimulates the formation of cAMP with an EC50 of 110 nM but is ineffective at inhibiting electrically stimulated dopamine release. [3]CGS 21680A is the hydrochloride salt, while CGS 21680C is the sodium salt of CGS 21680.
in vivo CGS 21680A is active p.o. in the spontaneously hypertensive rat at a dose of 10 mg/kg with efficacy for up to 24 hr. CGS 21680A caused a transient (60 min) increase in heart rate. [1]CGS 21680 is a potent depressant of the spontaneous, acetylcholine and glutamate evoked firing of rat cerebral cortical neurons. [4]

プロトコル(参考用のみ)

キナーゼアッセイ Radioligand binding
Binding to A2 receptors is measured in ADA-pretreated rat striatal membranes using [3H]NECA (specific activity, 20 Ci/mmol) in the presence of 50 nM cyclopentyladenosine to block A, receptors and in the presence of 100 μM 2-CADO to define nonspecific binding. Assay conditions are similar to those used to assess [3H]CHA binding except that the buffer also contained 10 mM MgC12. The final reaction volume is 2 ml with [3H]NECA being included at a final concentration of 2 nM.
動物実験 動物モデル rat
投薬量 10 mg/kg
投与方法 p.o.

カスタマーフィードバック

Data from [Data independently produced by , , Toxicol Appl Pharmacol, 2016, 289(1):109-16.]

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 is a tumor suppressor of NASH-associated hepatocellular carcinoma [ Cell Rep Med, 2023, 4(9):101188] PubMed: 37729873
Adenosine A2A receptor is a tumor suppressor of NASH-associated hepatocellular carcinoma [ Cell Rep Med, 2023, 4(9):101188] PubMed: 37729873
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
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
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
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
CD73-derived adenosine controls inflammation and neurodegeneration by modulating dopamine signalling. [ Brain, 2019, 142(3):700-718] PubMed: 30689733
Design, synthesis and biological evaluation of 2-hydrazinyladenosine derivatives as A2A adenosine receptor ligands [ Eur J Med Chem, 2019, 179:310-324] PubMed: 31255928
The cAMP-Adenosine Feedback Loop Maintains the Suppressive Function of Regulatory T Cells [ J Immunol, 2019, 203(6):1436-1446] PubMed: 31420466
A2A Receptor Activation Attenuates Hypertensive Cardiac Remodeling via Promoting Brown Adipose Tissue-Derived FGF21. [ Cell Metab, 2018, 28(3):476-489] PubMed: 30017353

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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