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CGS 21680 Hydrochloride

Catalog No. T6441 CAS 124431-80-7

Synonyms: CGS 21680 HCl

CGS 21680 Hydrochloride (CGS 21680 HCl)(IC50=22 nM), an adenosine receptor agonist, exhibits 140-fold potency in A2 receptor over A1 receptor.

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CGS 21680 Hydrochloride Chemical Structure

CGS 21680 Hydrochloride, CAS 124431-80-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
2 mg	In stock	$ 48.00
5 mg	In stock	$ 78.00
10 mg	In stock	$ 117.00
25 mg	In stock	$ 238.00
50 mg	In stock	$ 432.00
100 mg	In stock	$ 638.00
1 mL * 10 mM (in DMSO)	In stock	$ 92.00

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Purity: 98.81%

Purity: 98.65%

Purity: 96.74%

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Description	CGS 21680 Hydrochloride (CGS 21680 HCl)(IC50=22 nM), an adenosine receptor agonist, exhibits 140-fold potency in A2 receptor over A1 receptor.
Targets&IC50	A2 receptor: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]
Cell Research	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.

Synonyms	CGS 21680 HCl
Molecular Weight	535.98
Formula	C23H29N7O6·HCl
CAS No.	124431-80-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 53.6 mg/mL (100 mM)

References and Literature

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. 3. Lupica CR, et al. J Pharmacol Exp Ther, 1990, 252(3), 1134-1141. 4. Phillis JW, et al. Brain Res, 1990, 509(2), 328-30. 6. Zhang M, et al. Activation of the adenosine A2A receptor exacerbates experimental autoimmune neuritis in Lewis rats in association with enhanced humoral immunity. J Neuroimmunol. 2016 Apr 15;293:129-36.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Anti-Neurodegenerative Disease Compound Library Membrane Protein-targeted Compound Library Anti-COVID-19 Compound Library Anti-Alzheimer's Disease Compound Library Anti-Infection Compound Library Bioactive Compounds Library Max Neurotransmitter Receptor Compound Library Anti-Hypertension Compound Library Target-Focused Phenotypic Screening Library

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Keywords

CGS 21680 Hydrochloride 124431-80-7 GPCR/G Protein Neuroscience Adenosine Receptor CGS-21680 Inhibitor CGS-21680 Hydrochloride CGS 21680 HCl CGS 21680 inhibit CGS21680 CGS21680 Hydrochloride P1 receptor inhibitor

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