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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 manufacturers
- PA-8
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- $39.00
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2026-07-27
- CAS:878437-15-1
- Purity: 97.64%
- Supply Ability: 10g
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| | 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 Basic information |
| Product 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 | | Synonyms: | 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;2-Amino-5,8-dihydro-5-[3-methoxy-4-(2-propen-1-yloxy)phenyl]pyrido[2,3-d]pyrimidine-4,7(3H,6H)-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]-;2-amino-5-[3-methoxy-4-(prop-2-en-1-yloxy)phenyl]-1H,4H,5H,6H,7H,8H-pyrido[2,3-d]pyrimidine-4,7-dione;PA-8, 10 mM in DMSO;5-(4-(Allyloxy)-3-methoxyphenyl)-2-amino-5,8-dihydropyrido[2,3-d]pyrimidine-4,7(3H,6H)-dione | | CAS: | 878437-15-1 | | MF: | C17H18N4O4 | | MW: | 342.35 | | EINECS: | 825-313-7 | | Product Categories: | | | Mol File: | 878437-15-1.mol | ![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 Structure](CAS/20200119/GIF/878437-15-1.gif) |
| | 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 Chemical Properties |
| density | 1.44±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | Soluble in DMSO | | pka | 14.74±0.40(Predicted) | | form | Solid | | color | White to yellow |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | 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 Usage And Synthesis |
| Uses | PA-8 is a potent, selective and orally active PACAP type I (PAC1) receptor antagonist. PA-8 inhibits the phosphorylation of CREB induced by PACAP in PAC1-, but not VPAC1- or VPAC2-receptor. PA-8 also inhibits PACAP-induced cAMP elevation with an IC50 of 2 nM[1][2]. | | 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 | | References | [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. DOI:10.1124/jpet.117.245415
[2] Ichiro Takasaki, et al. The novel small-molecule antagonist of PAC1 receptor attenuates formalin-induced inflammatory pain behaviors in mice. J Pharmacol Sci. 2019 Feb;139(2):129-132. DOI:10.1016/j.jphs.2018.11.011 |
| | 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 Preparation Products And Raw materials |
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