PU 02

PU 02 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 with IC50 values ranging from 0.36 to 1.3 µM for human 5-HT3A, 5-HT3AB, 5-HT3AC, and 5-HT3AE in a FLIPR membrane potential assay using HEK293 cells expressing human recombinant receptors. It is selective for 5-HT3 over other Cys-loop containing receptors with IC50 values >100 µM for mouse, rat, and human nicotinic (nACh), human GABAA, and human glycine (Gly) receptors. PU 02 inhibits currents induced by 5-HT (Cay-14332) in COS-7 cells expressing human 5-HT3A (IC50 = 0.49 µM). PU 02 also reduces growth of HepG2 cells in a dose-dependent manner via induction of cell cycle arrest at the G2/M phase and apoptosis.Formal Name: 6-[(1-naphthalenylmethyl)thio]-9H-purine. CAS Number: 313984-77-9. Molecular Formula: C16H12N4S. Formula Weight: 292.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml. lambdamax: 224, 294 nm. SMILES: C12=NC=NC(SCC3=C(C=CC=C4)C4=CC=C3)=C1NC=N2. InChi Code: InChI=1S/C16H12N4S/c1-2-7-13-11(4-1)5-3-6-12(13)8-21-16-14-15(18-9-17-14)19-10-20-16/h1-7,9-10H,8H2,(H,17,18,19,20). InChi Key: BGMSTNYJYPSLHN-UHFFFAOYSA-N.