| Identification | Back Directory | [Name]
2-amino-5-[3-methoxy-4-(prop-2-en-1-yloxy)phenyl]-3H,4H,5H,6H,7H,8H-pyrido[2,3-d]pyrimidine-4,7-dione | [CAS]
878437-15-1 | [Synonyms]
2-Amino-5,8-dihydro-5-[3-methoxy-4-(2-propen-1-yloxy)phenyl]pyrido[2,3-d]pyrimidine-4,7(3H,6H)-dione
2-amino-5-[3-methoxy-4-(prop-2-en-1-yloxy)phenyl]-3H,4H,5H,6H,7H,8H-pyrido[2,3-d]pyrimidine-4,7-dione
Pyrido[2,3-d]pyrimidine-4,7(3H,6H)-dione, 2-amino-5,8-dihydro-5-[3-methoxy-4-(2-propen-1-yloxy)phenyl]- | [EINECS(EC#)]
825-313-7 | [Molecular Formula]
C17H18N4O4 | [MDL Number]
MFCD07400226 | [MOL File]
878437-15-1.mol | [Molecular Weight]
342.35 |
| Chemical Properties | Back Directory | [density ]
1.44±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
14.74±0.40(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Biological Activity]
PA-8 is a potent, selective, and orally active PACAP type I (PAC1) receptor antagonist. It inhibits PACAP-induced phosphorylation of CREB in PAC1 receptors, but not VPAC1 or VPAC2 receptors. It also inhibits PACAP-induced cAMP elevation with IC50 of 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. | [in vivo]
PA-8 (100 pmol/5 μL; intrathecal injection; once; male ddY mice) treatment inhibits PACAP-induced aversive responses and mechanical allodynia in vivo. | [storage]
Store at -20°C |
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