A selective 5-HT3 receptor antagonist
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PU 02

Item No. 14312

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    5 mg

    $94

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    10 mg

    $174

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    25 mg

    $412

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    50 mg

    $728

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    Cayman Chemical
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    Product Description

    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.1 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.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Trattnig, S.M., Harpsøe, K., Thygesen, S.B., et al. Discovery of a novel allosteric modulator of 5-HT3 receptors: inhibition and potentiation of Cys-loop receptor signaling through a conserved transmembrane intersubunit site. The Journal of Biological Chemisty 287(30), 25241-25254 (2012).

    2. Yang, X.-G., Bao, Y.-L., Huang, Y.-X., et al. 6-[(1-naphthylmethyl)sulfanyl]-9H-purine induces G2/M phase arrest and apoptosis in human hepatocellular carcinoma HepG2 cells. Eur. J. Pharmacol. 695(1-3), 27-33 (2012).