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-[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)
- CAS No.
- 878437-15-1
- Chemical 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
- 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;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;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;Pyrido[2,3-d]pyrimidine-4,7(3H,6H)-dione, 2-amino-5,8-dihydro-5-[3-methoxy-4-(2-propen-1-yloxy)phenyl]-
- CBNumber:
- CB04752103
- Molecular Formula:
- C17H18N4O4
- Molecular Weight:
- 342.35
- MDL Number:
- MFCD07400226
- MOL File:
- 878437-15-1.mol
- MSDS File:
- SDS
- TDS File:
- TDS
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H319-H315-H335 |
| Precautionary statements | P264-P280-P305+P351+P338-P337+P313P-P264-P280-P302+P352-P321-P332+P313-P362 |
| 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 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 42131 | PA-8 ≥98% | 878437-15-1 | 5mg | $43 | 2026-04-30 | Buy |
| Cayman Chemical | 42131 | PA-8 ≥98% | 878437-15-1 | 10mg | $82 | 2026-04-30 | Buy |
| Cayman Chemical | 42131 | PA-8 ≥98% | 878437-15-1 | 25mg | $183 | 2026-04-30 | Buy |
| Cayman Chemical | 42131 | PA-8 ≥98% | 878437-15-1 | 50mg | $323 | 2026-04-30 | Buy |
| Biosynth | DKB43715 | 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 | 878437-15-1 | 50mg | $677.5 | 2026-06-04 | Buy |
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, Uses, Production
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
Raw materials
Preparation Products
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 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| BOC Sciences | 1-631-485-4226; 16314854226 | info@bocsci.com | United States | 9920 | 65 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4860 | 55 | |
| Shanghai YuanYe Biotechnology Co., Ltd. | 15026964105 | 2881489226@qq.com | China | 89667 | 60 |
| Shanghai Chaolan Chemical Technology Center | QQ：65489617 13301690235 | Sales@ATKchemical.com | China | 9699 | 58 |
| Shanghai Hongye Biotechnology Co. Ltd | 400-9205774 400-920-5774 | sales@glpbio.cn | China | 6705 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 | marketing@targetmol.com | United States | 32431 | 58 |
| Changzhou Chenhong Biotechnology Co., Ltd. | +86-0519-85788828 +86-13775037613 | sales@chemrenpharm.com | China | 4058 | 58 |
| Suzhou Chenrui Biotechnology Co. LTD | 17625585511 | 1580084073@qq.com | China | 992 | 58 |
| ShangHai ChuanQian Chemcial Technique Centre | 15869524721 | 3525679403@qq.com | China | 4565 | 58 |
| Beijing Jin Ming Biotechnology Co., Ltd. | 010-60605840 | psaitong@jm-bio.com | China | 27626 | 58 |
