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CGS 15943 is an orally bioavailable non-xanthine antagonist at adenosine (A) receptors with IC50 values of 3.5, 4.2, 16, and 51 nM in CHO cells transfected with human recombinant A1, A2A, A2B, and A3 receptors, respectively.1,2 It also binds to the phosphatidylinositol 3-kinase (PI3K) catalytic subunit p110γ, and it inhibits proliferation of HCC hepatocellular carcinoma and PDAC pancreatic cancer adenocarcinoma cells through the PI3K/Akt signaling pathway.3 In rats, CGS 15943 (0.1-10 mg/kg, i.p.) increases locomotor activity in a dose-dependent manner.4 It also reinforces and reinstates cocaine-seeking in baboons through an adenosine-dependent mechanism.5
WARNING This product is not for human or veterinary use.
1. Adenosine receptors and their ligands. Naunyn-Schmiedeberg's Arch. Pharmacol. 362(4), 382-391 (2000).
2. Pharmacological characterization of CGS 15943A: a novel nonxanthine adenosine antagonist. J. Pharmacol. Exp. Ther. 242(3), 784-790 (1987).
3. Caffeine and the analog CGS 15943 inhibit cancer cell growth by targeting the phosphoinositide 3-
4. CGS 15943, a nonxanthine adenosine receptor antagonist: effects on locomotor activity of nontolerant and caffeine-
5. The adenosine receptor antagonist CGS15943 reinstates cocaine-