Product Details
| Product Name:
PA-8 |
CAS No.:
878437-15-1 |
| Purity:
97.64% |
Supply Ability:
10g |
| Release date:
2024/11/16 |
Product Introduction
Bioactivity
| 名稱 | PA-8 |
| 描述 | 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. |
| 體外活性 | 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]. |
| 體內(nèi)活性 | 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. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 22.5 mg/mL (65.7 mM), Sonication and heating to 60℃ are recommended.
|
| 關(guān)鍵字 | PA 8 | PA-8 | PA8 |
| 相關(guān)產(chǎn)品 | PACAP 1-38 acetate | PACAP (6-38), human, ovine, rat acetate | PAC1R antagonist 1 | PACAP-38 (31-38), human, mouse, rat acetate | PACAP-related Peptide (human) (trifluoroacetate salt) | PACAP (6-27) (human, chicken, mouse, ovine, porcine, rat) (trifluoroacetate salt) | PACAP (1-27), human, ovine, rat acetate | PACAP-related Peptide (rat) (trifluoroacetate salt) | PACAP (1-38), human, ovine, rat |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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