PW0787

SKU: orb1940198

Description

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

Key Properties

• CAS Number: 2624131-45-7
• MW: 460.433
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₀F₄N₄O₂
• SMILES: OCCNC(=O)c1cccc2N(CCc12)c1cc(Cc2cc(F)cc(c2)C(F)(F)F)ncn1
• Target: GPR
• Solubility: In Vitro: DMSO : 50 mg/mL (108.60 mM)

Bioactivity

• 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. 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. Animal model: Na ve 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

GPR