CGS 21680 HCl

Catalog No.S2153

For research use only.

CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor.

CGS 21680 HCl Chemical Structure

CAS No. 124431-80-7

Selleck's CGS 21680 HCl has been cited by 11 Publications

1 Customer Review

Purity & Quality Control

Choose Selective Adenosine Receptor Inhibitors

Biological Activity

Description CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor.
Targets
Adenosine A2 receptor [1]
(in rat brain tissue)
22 nM
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]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: rat
  • Dosages: 10 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(186.57 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+50%dd H2O
For best results, use promptly after mixing.

5 mg/mL

Chemical Information

Molecular Weight 535.98
Formula

C23H29N7O6.HCl

CAS No. 124431-80-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCNC(=O)C1C(C(C(O1)N2C=NC3=C(N=C(N=C32)NCCC4=CC=C(C=C4)CCC(=O)O)N)O)O.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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 ddH2O, 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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy CGS 21680 HCl | CGS 21680 HCl supplier | purchase CGS 21680 HCl | CGS 21680 HCl cost | CGS 21680 HCl manufacturer | order CGS 21680 HCl | CGS 21680 HCl distributor