THPP-1
- Product Name
- THPP-1
- CAS No.
- 1257051-63-0
- Chemical Name
- THPP-1
- Synonyms
- THPP-1;THPP-1, 10 mM in DMSO;PDE10A,SIMA,object,THPP 1,recognition,Phosphodiesterase (PDE),Inhibitor,inhibit,novel,THPP-1,THPP1;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;(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;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-
- CBNumber
- CB06127943
- Molecular Formula
- C23H21ClN6O3
- Formula Weight
- 464.9
- MOL File
- 1257051-63-0.mol
THPP-1 Property
- 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
N-Bromosuccinimide Price
- Product number
- CS-0066613
- Product name
- THPP-1
- Purity
- 98.95%
- Packaging
- 5mg
- Price
- $450
- Updated
- 2021/12/16
- Product number
- CS-0066613
- Product name
- THPP-1
- Purity
- 98.95%
- Packaging
- 10mg
- Price
- $750
- Updated
- 2021/12/16
- Product number
- CS-0066613
- Product name
- THPP-1
- Purity
- 98.95%
- Packaging
- 50mg
- Price
- $2250
- Updated
- 2021/12/16
- Product number
- CS-0066613
- Product name
- THPP-1
- Purity
- 98.95%
- Packaging
- 100mg
- Price
- $3350
- Updated
- 2021/12/16
THPP-1 Chemical Properties,Usage,Production
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
IC50: 1-1.3 nM (PDE10A).
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
Raw materials
Preparation Products
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