THPP-1 manufacturers
- THPP-1
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- $40.00
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2026-07-14
- CAS:1257051-63-0
- Purity: 99.46%
- Supply Ability: 10g
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| Product Name: | THPP-1 | | Synonyms: | THPP-1;PDE10A,SIMA,object,THPP 1,recognition,Phosphodiesterase (PDE),Inhibitor,inhibit,novel,THPP-1,THPP1;Methanone, [2-(6-chloro-3-pyridinyl)-7,8-dihydro-4-(2-methoxyethoxy)pyrido[4,3-d]pyrimidin-6(5H)-yl]imidazo[1,5-a]pyridin-1-yl-;2-chloro-5-(6-{imidazo[1,5-a]pyridine-1-carbonyl}-4-(2-methoxyethoxy)-5H,6H,7H,8H-pyrido[4,3-d]pyrimidin-2-yl)pyridine;THPP-1, 10 mM in DMSO;(2-(6-Chloropyridin-3-yl)-4-(2-methoxyethoxy)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)(imidazo[1,5-a]pyridin-1-yl)methanone | | CAS: | 1257051-63-0 | | MF: | C23H21ClN6O3 | | MW: | 464.9 | | EINECS: | | | Product Categories: | | | Mol File: | 1257051-63-0.mol |  |
| | THPP-1 Chemical Properties |
| density | 1.45±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO: 31.25 mg/mL (67.22 mM) | | form | A solid | | pka | 4.70±0.30(Predicted) | | color | Off-white to light yellow |
| | THPP-1 Usage And Synthesis |
| Uses | 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]. | | Biological Activity | THPP-1, a chemical probe recommended by SGC, is a potent and orally active inhibitor of phosphodiesterase 10A (PDE10A) with Ki values of 1 nM and 1.3 nM for human and rat, respectively. THPP-1 has good pharmacological properties. | | 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. |
| | target | | | IC 50 | PDE10 | | References | [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. DOI:10.1016/j.chembiol.2019.11.004
[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. DOI:10.1007/s00213-016-4290-1 |
| | THPP-1 Preparation Products And Raw materials |
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