Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
サンプルについてお問い合わせ | |||||
5 mg | 在庫あり | ¥ 9,000 | |||
10 mg | 在庫あり | ¥ 16,500 | |||
25 mg | 在庫あり | ¥ 35,500 | |||
50 mg | 在庫あり | ¥ 62,500 | |||
100 mg | 在庫あり | ¥ 110,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 10,000 |
説明 | 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. |
ターゲット&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. |
分子量 | 342.35 |
分子式 | C17H18N4O4 |
CAS No. | 878437-15-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 22.5 mg/mL (65.7 mM), Sonication and heating to 60℃ are recommended.
You can also refer to dose conversion for different animals. 詳細
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
PA-8 878437-15-1 GPCR/G Protein PACAP PA 8 PA8 Inhibitor inhibitor inhibit