PA 8

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Cat.No. 6657 - PA 8 | C17H18N4O4 | CAS No. 878437-15-1
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
Reviews
Literature

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
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

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

Preparing Stock Solutions

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.

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

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


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Keywords: PA 8, PA 8 supplier, PA8, Pituitary, adenylate, cyclase-activating, polypeptide, PACAP, receptors, antagonists, antagonism, PAC1, analgesics, analgesia, Receptors, 6657, Tocris Bioscience

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