A selective 5-HT3 receptor antagonist (IC50s = 0.36-1.3 μM for human 5-HT3A

PU 02 – 50 mg

Brand:
Cayman
CAS:
313984-77-9
Storage:
-20
UN-No:
Non-Hazardous - /

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.{38330} 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 (Item No. 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.{38329}  

 

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Description

A selective 5-HT3 receptor antagonist (IC50s = 0.36-1.3 μM for human 5-HT3A, 5-HT3AB, 5-HT3AC, and 5-HT3AE in a FLIPR membrane potential assay); selective for 5-HT3 over other Cys-loop containing receptors (IC50 values >100 μM for mouse, rat, and human nAChRs, human GABAARs, and human GlyRs; inhibits 5-HT-induced currents in COS-7 cells expressing human 5-HT3A (IC50 = 0.49 μM); reduces growth of HepG2 cells in a dose-dependent manner ,

Formal name: 6-[(1-naphthalenylmethyl)thio]-9H-purine

Synonyms: 

Molecular weight: 292.4

CAS: 313984-77-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Cancer|Cell Cycle|G2/M||Research Area|Cancer|Cell Death|Apoptosis

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