[CAS NO. 1436004-46-4] PA-9
PRODUCTS SPECIFICATIONS [1436004-46-4]
DESCRIPTION [1436004-46-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 338.36 |
| Molecular Formula | C17H18N6O2 |
| SMILES | O=C(C(C1)CN(C2=NNC3=C2C=CC=C3)C1=O)NCCC4=CN=CN4 |
Summary
PA-9 is a pituitary adenylate cyclase-activating polypeptide (PACAP) type I ( PAC1 ) receptor antagonist. PA-9 dose dependently inhibits PACAP-induced cAMP elevation with an IC 50 of 5.6 nM. PA-9 can be used for the research of neuropathic and/or inflammatory pain [1] .
IC50 & Target
|
PAC1 receptor |
In Vitro
PA-9 (10 pM to 10 nM; 30 minutes) dose dependently inhibits PACAP-induced (1 nM) CREB phosphorylation in the CHO cells expressing PAC1 receptors [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PA-9 (100 pmol; co-injection with PACAP) attenuates the development of PACAP-induced (100 pmol/5 μL; intrathecal injection) aversive responses of mice
[1]
.
PA-9 (100 pmol; co-injection with PACAP) significantly blocks the induction of PACAP-induced (100 pmol) mechanical allodynia
[1]
.
PA-9 (100 pmol/5 μl; single intrathecal injection alone) does not induce aversive responses and mechanical allodynia of mice
[1]
.
PA-9 is well accommodated in the subpocket formed by L80, F81, I83, G91, V92, P107, A112, and C113 of the PAC1 receptor, precipitating in hydrophobic interactions
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male ddY mice (6 weeks old at the start of experiments; intrathecal injection 100 pmol/5 μL PACAP) [1] |
| Dosage: | intrathecal injection, co-injection with PACAP. |
| Administration: | 100 pmol/5 μL |
| Result: |
Attenuated the development of PACAP-induced aversive responses.
Blocked the induction of PACAP-induced mechanical allodynia. |
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
DMSO : 250 mg/mL ( 738.86 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.9554 mL | 14.7772 mL | 29.5543 mL |
| 5 mM | 0.5911 mL | 2.9554 mL | 5.9109 mL |
| 10 mM | 0.2955 mL | 1.4777 mL | 2.9554 mL |