A PAC1 receptor antagonist
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PA-8

Item No. 42131

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal 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
CAS Number
878437-15-1
Molecular Formula
C17H18N4O4
Formula Weight
342.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
C=CCOC(C=C1)=C(OC)C=C1C(C2)C3=C(NC(N)=NC3=O)NC2=O
InChi Code
InChI=1S/C17H18N4O4/c1-3-6-25-11-5-4-9(7-12(11)24-2)10-8-13(22)19-15-14(10)16(23)21-17(18)20-15/h3-5,7,10H,1,6,8H2,2H3,(H4,18,19,20,21,22,23)
InChi Key
DCSWTWUTSKSXOV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $43

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    10 mg

    $82

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    25 mg

    $183

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    50 mg

    $323

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    Product Description

    PA-8 is a pituitary adenylate cyclase-activating peptide (PACAP) type 1 (PAC1) receptor antagonist.1 It selectively inhibits PACAP-induced CREB phosphorylation in CHO cells expressing the PAC1 receptor over CHO cells expressing vasoactive intestinal polypeptide receptor 1 (VPAC1) or VPAC2 at 10 nM. PA-8 inhibits PACAP-induced cAMP accumulation in CHO cells expressing the PAC1 receptor (IC50 = 2 nM). Intrathecal administration of PA-8 (100 pmol/animal) reduces PACAP-induced transient aversive behaviors and mechanical allodynia in mice.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Takasaki, I., Watanabe, A., Yokai, M., et al. In silico screening identified novel small-molecule antagonists of PAC1 receptor. J. Pharmacol. Exp. Ther. 365(1), 1-8 (2018).