[CAS NO. 878437-15-1] PA-8

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PRODUCTS SPECIFICATIONS [878437-15-1]

Catalog

HY-133529

Brand

MCE

CAS

878437-15-1

DESCRIPTION [878437-15-1]

Overview

MDL	-
Molecular Weight	342.35
Molecular Formula	C17H18N4O4
SMILES	O=C1C(C(C2=CC=C(OCC=C)C(OC)=C2)CC(N3)=O)=C3N=C(N)N1

For research use only. We do not sell to patients.

Summary

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 IC ₅₀ of 2 nM ^[1] ^[2] .

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 ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 ^[1] .
PA-8 (3-30 mg/kg, p.o.) treatment results in the dose-dependent attenuation of the second phase of formalin-induced nociceptive responses. PA-8 also inhibits c-fos upregulation in the ipsilateral dorsal horn of the spinal cord ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male ddY mice (6 weeks old) injected with PACAP (100 pmol) ^[1]
Dosage:	100 pmol/5 µL
Administration:	Intrathecal injection; once
Result:	Inhibited PACAP-induced aversive responses and mechanical allodynia in vivo.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL ( 73.02 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.9210 mL	14.6049 mL	29.2099 mL
5 mM	0.5842 mL	2.9210 mL	5.8420 mL
10 mM	0.2921 mL	1.4605 mL	2.9210 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (7.30 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

Pyrido[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(1H,6H)-dione, 2-amino-5,8-dihydro-5-[3-methoxy-4-(2-propenyloxy)phenyl]-

2-Amino-5,8-dihydro-5-[3-methoxy-4-(2-propen-1-yloxy)phenyl]pyrido[2,3-d]pyrimidine-4,7(3H,6H)-dione