A potent adenosine receptor antagonist
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CGS 15943

Item No. 22073

Technical Information
Formal Name
9-chloro-2-(2-furanyl)-[1,2,4]triazolo[1,5-c]quinazolin-5-amine
CAS Number
104615-18-1
Synonyms
  • CGS 15943A
Molecular Formula
C13H8ClN5O
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
DMF: 1 mg/mlDMF:PBS (pH 7.2)(1:3): 0.25 mg/mlDMSO: 0.5 mg/ml
λmax
260 nm
SMILES
ClC1=CC=C(C2=C1)N=C(N)N3C2=NC(C4=CC=CO4)=N3
InChi Code
InChI=1S/C13H8ClN5O/c14-7-3-4-9-8(6-7)12-17-11(10-2-1-5-20-10)18-19(12)13(15)16-9/h1-6H,(H2,15,16)
InChi Key
MSJODEOZODDVGW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    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.

    References & Product Citations
    Product Description References

    1. Klotz, K.-N. Adenosine receptors and their ligands. Naunyn-Schmiedeberg's Arch. Pharmacol. 362(4), 382-391 (2000).

    2. Ghai, G., Francis, J.E., Williams, M., et alPharmacological characterization of CGS 15943A: a novel nonxanthine adenosine antagonist. J. Pharmacol. Exp. Ther. 242(3), 784-790 (1987).

    3. Edling, C.E., Selvaggi, F., Ghonaim, R., et alCaffeine and the analog CGS 15943 inhibit cancer cell growth by targeting the phosphoinositide 3-kinase/Akt pathway. Cancer Biol. Ther. 15(5), 524-532 (2014).

    4. Holtzman, S.G. CGS 15943, a nonxanthine adenosine receptor antagonist: effects on locomotor activity of nontolerant and caffeine-tolerant rats. Life Sci. 49(21), 1563-1570 (1991).

    5. Weerts, E.M., and Griffiths, R.R. The adenosine receptor antagonist CGS15943 reinstates cocaine-seeking behavior and maintains self-administration in baboons. Psychopharmacology (Berl) 168(1-2), 155-163 (2003).