878437-15-1
PA-8
CAS: 878437-15-1
Molecular Formula: C17H18N4O4
878437-15-1 - Names and Identifiers
878437-15-1 - Physico-chemical Properties
| Molecular Formula | C17H18N4O4 |
| Molar Mass | 342.35 |
| Density | 1.44±0.1 g/cm3(Predicted) |
| Appearance | Solid |
| pKa | 14.74±0.40(Predicted) |
| Storage Condition | 2-8°C，密封，干燥 |
| In vitro study | 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. |
878437-15-1 - Reference Information
| biological activity | PA-8 is a potent, selective, orally active PACAP type I (PAC1) receptor antagonists. PA-8 inhibits PACAP-induced phosphorylation of CREB in the PAC1 receptor, but does not inhibit VPAC1 or VPAC2 receptors. PA-8 also inhibited PACAP-induced cAMP elevation with an IC50 of 2 nM. |
| Animal Model: | Male ddY mice (6 weeks old) injected with PACAP (100 pmol) |
| Dosage: | 100 pmol/5 µL |
| Administration: | Intrathecal injection; once |
| Result: | Inhibited PACAP-induced aversive responses and mechanical allodynia in vivo. |
Last Update：2024-04-09 21:04:16
