PA 8

Catalog # Availability Size / Price Qty
6657/10
6657/50
Cat.No. 6657 - PA 8 | C17H18N4O4 | CAS No. 878437-15-1
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Description: PAC1 receptor antagonist

Chemical Name: 2-Amino-5,8-dihydro-5-[3-methoxy-4-(2-propen-1-yloxy)phenyl]pyrido[2,3-d]pyrimidine-4,7(3H,6H)-dione

Purity: ≥98%

Product Details
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Biological Activity

PAC1 receptor antagonist. Inhibits PACAP-induced CREB phosphorylation in PAC1, but not VPAC1 or VPAC2, expressing cells. Also inhibits PACAP-induced increases in cAMP levels in vitro (IC50 = 2 nM) and PACAP-induced aversive responses and mechanical allodynia following intrathecal injection in vivo.

Technical Data

M.Wt:
342.35
Formula:
C17H18N4O4
Solubility:
Soluble to 50 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
878437-15-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. In silico screening identified novel small-molecule antagonists of PAC1 receptor.
    Takasaki et al.
    J.Pharmacol.Exp.Ther., 2018;365:1

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