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PA 8

Cat. No. 6657 1 Citation Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
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% (HPLC)
Datasheet
Citations (1)
Reviews
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for PA 8

PA 8 is a 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.

Compound Libraries for PA 8

PA 8 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for PA 8

M. Wt 342.35
Formula C17H18N4O4
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 878437-15-1
PubChem ID 6485327
InChI Key DCSWTWUTSKSXOV-UHFFFAOYSA-N
Smiles COC1=C(C=CC(C2CC(NC3=C2C(N=C(N3)N)=O)=O)=C1)OCC=C

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.

Solubility Data for PA 8

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 17.12 50

Preparing Stock Solutions for PA 8

The following data is based on the product molecular weight 342.35. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 5.84 mL 29.21 mL 58.42 mL
2.5 mM 1.17 mL 5.84 mL 11.68 mL
5 mM 0.58 mL 2.92 mL 5.84 mL
25 mM 0.12 mL 0.58 mL 1.17 mL

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References for PA 8

References are publications that support the biological activity of the product.

Takasaki et al (2018) In silico screening identified novel small-molecule antagonists of PAC1 receptor. J.Pharmacol.Exp.Ther. 365 1 PMID: 29363578

If you know of a relevant reference for PA 8, please let us know.

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1 Citation for PA 8

Citations are publications that use Tocris products. Selected citations for PA 8 include:

Varodayan et al (2020) PACAP regulation of central amygdala GABAergic synapses is altered by restraint stress. Neuropharmacology 168 PMID: 31476352

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