CGS 15943

SKU: orb1308459

Description

CGS 15943 is a potent, orally active non-xanthine adenosine receptor antagonist with high affinity for human A1 (Ki=3.5 nM) and A2A (Ki=4.2 nM) receptors. It is widely used as a pharmacological tool in vitro and in vivo to study adenosine signaling in research areas such as cardiovascular function, neuroprotection, and inflammation.

Research Area

Neuroscience, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 104615-18-1
• MW: 285.69
• Purity: 99.63% (May vary between batches)
• Formula: C₁₃H₈ClN₅O
• SMILES: Nc1nc2ccc(Cl)cc2c2nc(nn12)-c1ccco1
• Target: PI3K,Adenosine Receptor
• Solubility: DMSO:12.22 mg/mL (42.77 mM);10% DMSO+90% Corn Oil:1 mg/mL (3.5 mM)

Bioactivity

• Target IC50:
  A3 receptor:51 nM (ki)|p110γ:1.1 μM|A2A receptor:4.2 nM (ki)|A1 receptor:3.5 nM (ki)|p110δ:8.47 μM|A2B receptor:16 nM (ki)
• In Vitro:
  CGS 15943 inhibits the kinase activity of the class IB PI3K isoform p110γ (IC50: 1.1 μM). CGS 15943 shows slight inhibition on p110δ (IC50: 8.47 μM). CGS 15943 (0-20 μM; 24 hours) reduces the phosphorylation of Akt at its residues Ser473 and Thr308 in HLF and Sk-Hep-1 cells. CGS 15943 (0-20 μM; 72 hours) inhibits growth of HLF and SK-Hep-1 cells, as well as HepG2 and PLC-PRF-5 cells.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, p110δ, p110γ, P1 receptor, Inhibitor, CGS 15943, CGS15943, CGS-15943, AdenosineReceptor, adenosine A2B receptor, adenosine A3 receptor, adenosine A1 receptor, adenosine A2A receptor, Adenosine Receptor, A3, A2A, A2B, A1, Phosphoinositide 3-kinase, PI3K

Compound Identifiers

PubChem CID

2690