1. GPCR/G Protein
  2. Adenosine Receptor
  3. CGS 21680 Hydrochloride

CGS 21680 Hydrochloride 

製品番号: HY-13201A 純度: 99.70%
取扱説明書

CGS 21680 Hydrochloride is a selective adenosine A2A receptor agonist with a Ki of 27 nM.

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CGS 21680 Hydrochloride 構造式

CGS 21680 Hydrochloride 構造式

CAS 番号 : 124431-80-7

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1  mL in DMSO USD 133 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 113 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 151 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 624 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 1080 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Other Forms of CGS 21680 Hydrochloride:

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製品説明

CGS 21680 Hydrochloride is a selective adenosine A2A receptor agonist with a Ki of 27 nM.

IC50 & Target

Ki: 27 nM (Adenosine A2A receptor)[5]

体外実験

CGS21680 significantly upregulates CD39 and CD73 expression. CGS21680 accelerates the adenosine triphosphate (ATP) hydrolysis and adenosine generation[1]. CGS21680 (10 nM) alone shows only small survival activity, but the activity is significantly enhanced by the addition of a phosphodiesterase inhibitor, IBMX. The survival activity of CGS21680 on cultured motoneurons is exerted by mixed effects of the adenylate cyclase-cAMP-PKA pathway and the transactivation of neurotrophin receptors[4].

体内実験

CGS21680 (1 mg/kg/i.p.) intervention promotes the development of EAN. CGS21680 exacerbates experimental autoimmune neuritis in Lewis rats induced with bovine peripheral myelin. The exacerbation is accompanied with reduced CD4+ Foxp3+ T cells, increased CD4+ CXCR5+ T cells, B cells, dendritic cells and antigen-specific autoantibodies, which is possibly due to the inhibition of IL-2 induced by CGS21680[2]. CGS21680 (0.1 mg/kg, i.p.) transiently increases heart frequency but does not modify blood pressure of rat, and does not modify either heart frequency or blood pressure at 0.01 mg/kg. Following transient MCAo, CGS21680 at both doses protects from neurological deficit from the first day up to 7 days thereafter. At this time, it has reduced microgliosis, astrogliosis and improved myelin organization in the striatum and cytoarchitecture of the ischemic cortex and striatum. Two days after transient MCAo, CGS21680 has reduced the number of infiltrated granulocytes into the ischemic tissue[3].

分子量

535.98

分子式

C₂₃H₃₀ClN₇O₆

CAS 番号

124431-80-7

SMILES

O=C(O)CCC1=CC=C(CCNC2=NC3=C(N=CN3[[email protected]]4[[email protected]](O)[[email protected]](O)[[email protected]@H](C(NCC)=O)O4)C(N)=N2)C=C1.Cl

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 20 mg/mL (37.31 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8657 mL 9.3287 mL 18.6574 mL
5 mM 0.3731 mL 1.8657 mL 3.7315 mL
10 mM 0.1866 mL 0.9329 mL 1.8657 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献
細胞実験
[2]

10×106 MNCs from each group are re-suspended in 2 mL RPMI 1640. Cell suspensions are added with carboxy-fluorescein diacetate, succinimidyl ester (CFSE, final concentration 2.5 μM) and thoroughly mixed. After incubation in the dark for 15 min at 37°C, the staining process is quenched by adding 10 mL ice-cold complete RPMI 1640 (containing 10% FBS) and incubated on ice for 5 min. Then cells are washed twice with RPMI 1640. Cell pellets are re-suspended in complete RPMI 1640 (containing 10% FBS). The stained MNCs (1×106 cells/mL, 1 mL/well) are cultured in triplicates in 24-well culture plates in the dark at 37°C. Each well is supplied with 50 μL of Concanavalin A (ConA, final concentration 5 μg/mL) or 50 μL of P0 peptide (final concentration 10 μg/mL). 72 h later, cells are collected and stained with PE-labeled anti-rat CD4 antibody for 30 min at 4°C. Finally, cells are analyzed with a flow cytometer.

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[2]

Female Lewis rats aged 6-8 weeks (body weight, 140-160 g) are housed under specific pathogen-free conditions in the local animal facility with free access to water and food. Administration of CGS21680 (at a dose of 1 mg/kg in PBS) starts on day 5 p.i. Rats in experimental group are injected with CGS21680 intraperitoneally (i.p.) every two days until the end of the experiments. Rats in control group are given equal volume of PBS in the same way. The doses (1 mg/kg/i.p.) and the treatment regimen (every two days, start on day 5 p.i.) are determined.

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献

純度: 99.70%

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Keywords:

CGS 21680CGS21680CGS-21680Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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製品名:
CGS 21680 Hydrochloride
製品番号:
HY-13201A
数量:
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