Shopping Cart
- Remove All
![TargetMol](https://www.targetmol.com/storage/error/oops.webp)
Your shopping cart is currently empty
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $39 | In Stock | |
10 mg | $72 | In Stock | |
25 mg | $155 | In Stock | |
50 mg | $272 | In Stock | |
100 mg | $478 | In Stock | |
1 mL x 10 mM (in DMSO) | $43 | In Stock |
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. |
Targets&IC50 | cAMP:2 nM |
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. |
Molecular Weight | 342.35 |
Formula | C17H18N4O4 |
Cas No. | 878437-15-1 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 22.5 mg/mL (65.7 mM), Sonication and heating to 60℃ are recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
|
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.