[CAS NO. 2624131-45-7] PW0787
PRODUCTS SPECIFICATIONS [2624131-45-7]
DESCRIPTION [2624131-45-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 460.42 |
| Molecular Formula | C23H20F4N4O2 |
| SMILES | O=C(C1=CC=CC2=C1CCN2C3=NC=NC(CC4=CC(F)=CC(C(F)(F)F)=C4)=C3)NCCO |
Summary
IC50 & Target
EC50: 135 nM (GPR52) [1]
In Vivo
PW0787 (0.3, 1, 3, or 10 mg/kg; IP) displays antipsychotic-like activity by significantly inhibiting amphetamine-induced hyperlocomotor behavior in mice
[1]
.
PW0787 is evaluated in rats after a single dose of 20 mg/kg by oral (PO) or 10 mg/kg by intravenous (IV) administration. PW0787 has excellent plasma exposure after PO (AUC
0-inf
= 13,749 ng•h/mL) and IV dosing (AUC
0-inf
=9030 ng•h/mL), as well as high maximum serum concentration following PO (C
max
=3407 ng/mL) and IV administration (C
max
=6726 ng/mL). Additionally, PW0787 displays good volume of plasma distribution (V
ss
=1.5 L/kg) and acceptable plasma clearance (CL=1.1 L/h/kg) after 10 mg/kg IV. Excellent oral bioavailability (F) with the value of 76% is observed
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Naïve male C57/BL6 mice weighing between 24 and 31 g |
| Dosage: | 0.3, 1, 3, or 10 mg/kg (dissolved in 0.9% saline containing 20% HP-β-CD with a final pH of the solution adjusted to 7.4) |
| Administration: | IP |
| Result: | Suppressed amphetamine (AMPH)-induced horizontal activity at both 3 mg/kg and 10 mg/kg doses. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 50 mg/mL ( 108.60 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1719 mL | 10.8596 mL | 21.7193 mL |
| 5 mM | 0.4344 mL | 2.1719 mL | 4.3439 mL |
| 10 mM | 0.2172 mL | 1.0860 mL | 2.1719 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution