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

CGS 21680 Hydrochloride 

Cat. No.: HY-13201A Purity: 99.70%
Handling Instructions

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

For research use only. We do not sell to patients.

CGS 21680 Hydrochloride Chemical Structure

CGS 21680 Hydrochloride Chemical Structure

CAS No. : 124431-80-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 133 In-stock
Estimated Time of Arrival: December 31
5 mg USD 113 In-stock
Estimated Time of Arrival: December 31
10 mg USD 151 In-stock
Estimated Time of Arrival: December 31
50 mg USD 624 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1080 In-stock
Estimated Time of Arrival: December 31
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Other Forms of CGS 21680 Hydrochloride:

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  • Biological Activity

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  • References

Description

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]

In Vitro

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].

In Vivo

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].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 20 mg/mL (37.31 mM)

*"≥" 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.
In Vivo:
  • 1.

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

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

  • 2.

    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

  • 3.

    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

*All of the co-solvents are provided by MCE.
References
Cell Assay
[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 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[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 has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

535.98

Formula

C₂₃H₃₀ClN₇O₆

CAS No.

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

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.70%

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Product Name:
CGS 21680 Hydrochloride
Cat. No.:
HY-13201A
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CGS 21680 Hydrochloride

Cat. No.: HY-13201A