THPP-1

SKU: orb1298874

Description

THPP-1 is a highly potent, orally bioavailable PDE10A inhibitor with Ki values of 1 nM (human) and 1.3 nM (rat). This small molecule is a valuable research tool for investigating PDE10A function in neuropsychiatric disorders, enabling both in vitro biochemical assays and in vivo pharmacological studies.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1257051-63-0
• MW: 464.9
• Purity: 99.46% (May vary between batches)
• Formula: C₂₃H₂₁ClN₆O₃
• SMILES: COCCOc1nc(nc2CCN(Cc12)C(=O)c1ncn2ccccc12)-c1ccc(Cl)nc1
• Target: PDE
• Solubility: DMSO:31 mg/mL (66.68 mM)

Bioactivity

• Target IC50:
  PDE10A:1-1.3 nM
• In Vivo:
  Consistent with rodent data, both THPP-1 and risperidone significantly attenuated the stimulant effects in SIMA when administered alone, though some differences were noted. Combination therapy with a low dose of risperidone produced significantly more robust effects. THPP-1 and risperidone also produced a marked reduction of wake cycle time and gamma frequency power in EEG. However, THPP-1 differed from risperidone by reducing spectral power of lower frequencies.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

novel, inhibit, object, PDE10A, Inhibitor, THPP 1, THPP1, THPP-1, SIMA, recognition, Phosphodiesterase (PDE), phosphodiesterase

Compound Identifiers

PubChem CID

49821991