1. GPCR/G Protein
  2. GPR52
  3. PW0787

PW0787 

Cat. No.: HY-138639 Purity: 99.18%
COA Handling Instructions

PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM). PW0787 suppresses psychostimulant behavior.

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

PW0787 Chemical Structure

PW0787 Chemical Structure

CAS No. : 2624131-45-7

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM). PW0787 suppresses psychostimulant behavior[1].

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 (AUC0-inf = 13,749 ng•h/mL) and IV dosing (AUC0-inf=9030 ng•h/mL), as well as high maximum serum concentration following PO (Cmax=3407 ng/mL) and IV administration (Cmax=6726 ng/mL). Additionally, PW0787 displays good volume of plasma distribution (Vss=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.
Molecular Weight

460.42

Formula

C23H20F4N4O2

CAS No.
SMILES

O=C(C1=CC=CC2=C1CCN2C3=NC=NC(CC4=CC(F)=CC(C(F)(F)F)=C4)=C3)NCCO

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
In Vitro: 

DMSO : 50 mg/mL (108.60 mM; Need ultrasonic)

Preparing
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
*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 (5.43 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

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

Purity: 99.18%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
PW0787
Cat. No.:
HY-138639
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