CGS 21680, adenosine A2 receptor agonist.

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

Product information

CAS Number: 120225-54-9

Molecular Weight: 499.52

Formula: C23H29N7O6

Chemical Name: 3-{4-[2-({6-amino-9-[(2R, 3R, 4S, 5S)-5-(ethylcarbamoyl)-3, 4-dihydroxyoxolan-2-yl]-9H-purin-2-yl}amino)ethyl]phenyl}propanoic acid

Smiles: CCNC(=O)[C@H]1O[C@H]([C@H](O)[C@@H]1O)N1C=NC2=C(N)N=C(NCCC3=CC=C(CCC(O)=O)C=C3)N=C12

InChiKey: PAOANWZGLPPROA-RQXXJAGISA-N

InChi: InChI=1S/C23H29N7O6/c1-2-25-21(35)18-16(33)17(34)22(36-18)30-11-27-15-19(24)28-23(29-20(15)30)26-10-9-13-5-3-12(4-6-13)7-8-14(31)32/h3-6,11,16-18,22,33-34H,2,7-10H2,1H3,(H,25,35)(H,31,32)(H3,24,26,28,29)/t16-,17+,18-,22+/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 100 mg/mL(186.57 mM). Water: Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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. 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. 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. CGS 21680 is a potent depressant of the spontaneous, acetylcholine and glutamate evoked firing of rat cerebral cortical neurons.

References:

1. Lupica CR, et al. J Pharmacol Exp Ther, 1990, 252(3), 1134-1141.
2. Jarvis MF, et al. J Pharmacol Exp Ther, 1989, 251(3), 888-893.
3. Hutchison AJ, et al. J Pharmacol Exp Ther, 1989, 251(1), 47-55.

Products are for research use only. Not for human use.