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
- 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
- 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
- Formula Weight
- 342.35
- 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 Property
- 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
Safety
- WGK Germany
- WGK 3
- Storage Class
- 11 - Combustible Solids
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
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,Usage,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
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