THPP-1
Based on 1 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.75%
- No. CAS: 1257051-63-0
- Fòrmula: C23H21ClN6O3
- Peso molecular:464.90
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) THPP-1
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Actividad biológica
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PDE10 |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar Hannover rats ranging from 200 to 300 g[1].
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Dosage:0.1-1.0 mg/kg.
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Administration:P.O.
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Result:Showed novel object recognition.
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Animal Model:Eleven monkeyswere surgically implanted with subcutaneous telemetric devices to permit the simultaneous recording of electrocorticogram (ECoG), electrooculogram (EOG), and electromyogram (EMG) activit
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Dosage:1, 3, 10 mg/kg.
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Administration:P.O.
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Result:Significantly attenuated the stimulant effects in SIMA.
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Animal Model:Male Wistar Hannover rats ranging from 200 to 300 g[1].
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Dosage:1-30 mg/kg.
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Administration:P.O. (10% Tween 80/90% water) 2 h prior to tissue collection (Pharmacokinetic Analysis).
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Result:Dose-dependently increases phosphorylation of GluR1 S845.
Chemical Information
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No. CAS 1257051-63-0
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Appearance Solid
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Peso molecular 464.90
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Fòrmula C23H21ClN6O3
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Color Off-white to light yellow
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SMILES
O=C(C1=C2C=CC=CN2C=N1)N3CCC4=NC(C5=CC=C(N=C5)Cl)=NC(OCCOC)=C4C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175
Solvente y solubilidad
DMSO : 31.25 mg/mL (67.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Smith SM, et al. The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey. Neuropharmacology. 2013 Jan;64:215-23. [Content Brief]
[2]. Vardigan JD, et al. Behavioral and qEEG effects of the PDE10A inhibitor THPP-1 in a novel rhesus model of antipsychotic activity. Psychopharmacology (Berl). 2016 Jul;233(13):2441-50. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1510 mL | 10.7550 mL | 21.5100 mL | 53.7750 mL |
| 5 mM | 0.4302 mL | 2.1510 mL | 4.3020 mL | 10.7550 mL | |
| 10 mM | 0.2151 mL | 1.0755 mL | 2.1510 mL | 5.3775 mL | |
| 15 mM | 0.1434 mL | 0.7170 mL | 1.4340 mL | 3.5850 mL | |
| 20 mM | 0.1076 mL | 0.5378 mL | 1.0755 mL | 2.6888 mL | |
| 25 mM | 0.0860 mL | 0.4302 mL | 0.8604 mL | 2.1510 mL | |
| 30 mM | 0.0717 mL | 0.3585 mL | 0.7170 mL | 1.7925 mL | |
| 40 mM | 0.0538 mL | 0.2689 mL | 0.5378 mL | 1.3444 mL | |
| 50 mM | 0.0430 mL | 0.2151 mL | 0.4302 mL | 1.0755 mL | |
| 60 mM | 0.0359 mL | 0.1793 mL | 0.3585 mL | 0.8963 mL |
THPP-1 Related Classifications
HY-117604 Related Classifications
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