| Name | PA-8 |
| Description | PA-8 is a small molecule receptor antagonist for PACAP Type I (PAC1) that is selective, effective, and orally active. PA-8 inhibits PacAP-induced CREB phosphorylation at PAC1- receptors, but does not inhibit VPAC1- or vpac2 receptors. PA-8 also inhibited PacAP-induced elevation of cAMP levels in vitro (IC50 = 2 nM) and PacAP-induced aversive response and mechanical atopic pain after intrathecal injection in vivo. |
| In vitro | In PAC1/CHO cells, PA-8 (10 pM to 10 nM; 30 minutes) dose-dependently inhibits PACAP (1 nM)-induced CREB phosphorylation. In VPAC1/CHO and VPAC2/CHO cells, PACAP (1 nM) also induces CREB phosphorylation; however, PA-8 (10 pM to 10 nM) does not inhibit this effect [1]. |
| In vivo | Treatment with PA-8 (100 pmol/5 μL; via intrathecal injection; single dose; in male ddY mice) effectively suppresses PACAP-induced aversive reactions and mechanical allodynia in vivo [1]. Additionally, oral administration of PA-8 (3-30 mg/kg) leads to a dose-dependent reduction in the second phase of formalin-induced pain responses. PA-8 also significantly reduces c-fos expression in the spinal cord's ipsilateral dorsal horn [2]. This showcases PA-8's potential in mitigating nociceptive behaviors and neuronal activation in a PACAP-administered male ddY mouse model (6 weeks old; 100 pmol PACAP) [1], confirming its analgesic and anti-allodynic effects in vivo. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.84 mM), Sonication is recommended.
DMSO : 22.5 mg/mL (65.72 mM), Sonication and heating to 60℃ are recommended.
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| Keywords | PACAP type I | PA-8 | PA8 | PA 8 |
| Inhibitors Related | PACAP 1-38 acetate | PACAP (1-38) free acid | PAC1R antagonist 1 | PACAP-38 (31-38), human, mouse, rat acetate | PACAP (1-27), human, ovine, rat acetate | [D-p-Cl-Phe6,Leu17]-VIP | [Arg-15,20,21,Leu17]-PACAP-Gly-Lys-Arg-NH2 | PACAP (6-38), human, ovine, rat acetate | PACAP (6-38), human, ovine, rat | PACAP (6-38), human, ovine, rat TFA | PACAP (1-38), human, ovine, rat | PACAP (1-38), human, ovine, rat TFA |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Orally Active Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library |
United States
