1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. THPP-1

THPP-1 

Cat. No.: HY-117604
Handling Instructions

THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species.

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

THPP-1 Chemical Structure

THPP-1 Chemical Structure

CAS No. : 1257051-63-0

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Description

THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species[1].

IC50 & Target

IC50: 1-1.3 nM (PDE10A)[1].

In Vivo

THPP-1 (0.1-1.0 mg/kg, p.o.) shows novel object recognition in rats[1].
THPP-1 (p.o., 1-30 mg/kg) dose-dependently increases phosphorylation of GluR1 S845 in the rat striatum whereas the total levels of GluR1 in the striatum are not affected. Administration of THPP-1 also results in an associated increase in the pGluR1/GluR1 ratios at all doses examined in this study[1].
THPP-1 (1, 3, 10 mg/kg, p.o.) significantly attenuated the stimulant effects in stimulant-induced motor activity (SIMA) in monkey[2].

Animal Model: Male Wistar Hannover rats ranging from 200 to 300 g[1].
Dosage: 0.1-1.0 mg/kg.
Administration: P.O.
Result: Showed novel object recognition.
Animal Model: Eleven monkeyswere surgically implanted with subcutaneous telemetric devices to permit the simultaneous recording of electrocorticogram (ECoG), electrooculogram (EOG), and electromyogram (EMG) activit
Dosage: 1, 3, 10 mg/kg.
Administration: P.O.
Result: Significantly attenuated the stimulant effects in SIMA.
Animal Model: Male Wistar Hannover rats ranging from 200 to 300 g[1].
Dosage: 1-30 mg/kg.
Administration: P.O. (10% Tween 80/90% water) 2 h prior to tissue collection (Pharmacokinetic Analysis).
Result: Dose-dependently increases phosphorylation of GluR1 S845.
Molecular Weight

464.90

Formula

C₂₃H₂₁ClN₆O₃

CAS No.

1257051-63-0

SMILES

O=C(C1=C2C=CC=CN2C=N1)N3CCC4=NC(C5=CC=C(N=C5)Cl)=NC(OCCOC)=C4C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

THPP-1THPP1THPP 1Phosphodiesterase (PDE)SIMAPDE10AnovelobjectrecognitionInhibitorinhibitorinhibit

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