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PA-8

Catalog No. T41005 CAS 878437-15-1

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.

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PA-8, CAS 878437-15-1

Pack Size	Availability	Price/USD
5 mg	In stock	$ 39.00
10 mg	In stock	$ 72.00
25 mg	In stock	$ 155.00
50 mg	In stock	$ 272.00
100 mg	In stock	$ 478.00
1 mL * 10 mM (in DMSO)	In stock	$ 43.00

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Purity: 97.64%

Biological Description

Chemical Properties

Storage & Solubility Information

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 induced CREB phosphorylation; however, PA-8 (10 pM to 10 nM) does not inhibit PACAP (1 nM)-induced CREB phosphorylation [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

Solubility Information

DMSO: 22.5 mg/mL (65.7 mM), Sonication and heating to 60℃ are recommended.

References and Literature

1. Ichiro Takasaki, et al. In Silico Screening Identified Novel Small-molecule Antagonists of PAC1 Receptor. J Pharmacol Exp Ther. 2018 Apr;365(1):1-8. 2. Takasaki I, Nakamura K, Shimodaira A, et al. The novel small-molecule antagonist of PAC1 receptor attenuates formalin-induced inflammatory pain behaviors in mice. J Pharmacol Sci. 2019;139(2):129-13

Related compound libraries

This product is contained In the following compound libraries：

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Related Products

Related compounds with same targets

PACAP (1-27), human, ovine, rat acetate PACAP 1-38 acetate PACAP-related Peptide (rat) (trifluoroacetate salt) PAC1R antagonist 1 PACAP-38 (31-38), human, mouse, rat acetate PACAP-related Peptide (human) (trifluoroacetate salt) PACAP (6-38), human, ovine, rat acetate PACAP (1-38), human, ovine, rat

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Keywords

PA-8 878437-15-1 GPCR/G Protein PACAP PA 8 PA8 inhibitor inhibit

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