CGS 21680 HCl

Catalog No.S2153

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

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CGS 21680 HCl Chemical Structure

CGS 21680 HCl Chemical Structure
Molecular Weight: 535.98

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Product Information

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Product Description

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]
IC50 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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

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.

Animal Study: [1]

Animal Models rat
Formulation water
Dosages 10 mg/kg
Administration p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Hutchison AJ, et al. J Pharmacol Exp Ther, 1989, 251(1), 47-55.

[2] Jarvis MF, et al. J Pharmacol Exp Ther, 1989, 251(3), 888-893.

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Chemical Information

Download CGS 21680 HCl SDF
Molecular Weight (MW) 535.98
Formula

C23H29N7O6.HCl

CAS No. 124431-80-7
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 107 mg/mL (199.63 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W 30 mg/mL
* <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.
Chemical Name 3-(4-(2-(6-amino-9-((2R,3R,4S,5S)-5-(ethylcarbamoyl)-3,4-dihydroxy-tetrahydrofuran-2-yl)-9H-purin-2-ylamino)ethyl)phenyl)propanoic acid hydrochloride

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.

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