CS-114
PF-2545920
CAS: 1292799-56-4
Molecular Formula: C25H20N4O
CS-114 - Names and Identifiers
CS-114 - Physico-chemical Properties
| Molecular Formula | C25H20N4O |
| Molar Mass | 392.4525 |
| Storage Condition | -20℃ |
| In vitro study | PF-2545920 showed excellent potency and selectivity for PDE10A with an IC50 of 1.26 nM. |
| In vivo study | In male CF-1 mice, intraperitoneal administration of PF-2545920 at doses of 0.3,3, and 5 mg/kg resulted in significant increases in GluR1 phosphorylation levels of 3,5.4, and 4.1-fold, respectively. MP-10 treatment of rat striatal sections at a concentration of 1 μm for 30 minutes resulted in a significant 2-fold increase in the level of GluR1S845 phosphorylation at the cell surface without altering the total GluR1 at the cell surface. In male CF-1 mice, MP-10 intraperitoneal administration at doses of 0.3,3, and 5 mg/kg resulted in a statistically significant increase in CREBS133 phosphorylation by 3,4, and 2.6 times. Intraperitoneal administration of CF-1 at a dose of 3 mg/kg increased enkephalin and substance P mRNA levels in the striatum of MP-10 mice. MP-10 intraperitoneal administration at a dose of 0.3-1 mg/kg reduced the avoidance response with a significant therapeutic effect in the mouse CAR model. Mice treated with MP-10 at a dose of 0.03 mg/kg spent more time on meaningless matters than the social mice, and MP-10 also dose-dependently reduced spontaneous activity. In male CD-1 mice, PDE10A administered subcutaneously at a dose of 1 mg/kg increased striatal cGMP 3-fold, PDE10A administered subcutaneously at a dose of 3.2 mg/kg produced approximately a 5-fold maximum increase in striatal cGMP. In Sprague-Dawley rats, PDE10A showed a clearance of 36 ml/min/kg at a dose of 0.1 mg/Kg, intravenous injection of DE10A at a dose of 0.3 mg/kg showed a clearance of 7.2/min/Kg in vivo, with an appropriate volume distribution volume, intravenous injection of DE10A at a dose of 0.03 mg/kg showed a clearance of 13.9/min/Kg in vivo with an appropriate volume of distribution. In the Sprague-Dawley rat physical conditioned avoidance response (CAR) test, PDE10A was active at concentrations significantly below total plasma exposure (115 nM) with an ED50 of 1 mg/kg. |
CS-114 - Reference Information
| biological activity | Mardepodect (PF-2545920) is an effective and selective PDE10A inhibitor with IC50 of 0.37 nM, which is more than 1000 times higher than the selectivity for PDE. |
| target | TargetValue PDE10A (Cell-free assay) 0.37 nM |
| Target | Value |
| PDE10A (Cell-free assay) | 0.37 nM |
| in vitro study | PF-2545920 showed excellent efficacy and selectivity for PDE10A, with IC50 of 1.26 nM. |
| in vivo study | in male CF-1 mice, PF-2545920 administered intraperitoneally at doses of 0.3,3, and 5 mg/kg, causing a significant increase in GluR1 phosphorylation level by 3,5.4, and 4.1 times, respectively. The phosphorylation level of GluR1S845 on the cell surface was significantly increased by 2 times without changing the total GluR1 on the cell surface after being treated with 1 μM MP-10 for 30 minutes. In male CF-1 mice, intraperitoneal administration of MP-10 at doses of 0.3,3, and 5 mg/kg resulted in statistically significant increases in CREBS133 phosphorylation by 3,4, and 2.6 times, respectively. In the striatum of CF-1 mice, intraperitoneal administration at a dose of 3 mg/kg was MP-10 to increase the level of enkephalin and substance P mRNA. MP-10 Intraperitoneal administration at a dose of 0.3-1 mg/kg reduces evasive response and has significant therapeutic effect in mouse CAR model. MP-10-treated mice at a dose of 0.03 mg/kg spent more time on meaningless things than gregarious mice, MP-10 also dose-dependently reduced spontaneous activity. In male CD-1 mice, subcutaneous administration of PDE10A at a dose of 1 mg/kg increased cGMP in striatum by a factor of 3, while subcutaneous administration of PDE10A at a dose of 3.2 mg/kg increased cGMP in striatum by a factor of about 5. In Sprague-Dawley rats, PDE10A showed a clearance rate of 36 ml/min/Kg by intravenous injection at a dose of 0.1 mg/kg. In Dog Beagle, DE10A showed a clearance rate of 7.2 ml/min/Kg by intravenous injection at a dose of 0.3 mg/kg, accompanied by appropriate volume distribution volume, in rhesus monkeys, DE10A, injected intravenously at a dose of 0.03 mg/kg, exhibits a clearance rate of 13.9 ml/min/Kg in vivo, accompanied by an appropriate volume distribution volume. In the Sprague-Dawley rat conditioned avoidance response test (CAR), PDE10A was active at a concentration significantly lower than the total plasma exposure (115 nM), with an ED50 of 1 mg/kg. |
Last Update：2024-04-09 19:05:04
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Product Name: Quinoline, 2-?[[4-?[1-?(methyl-?11C)?-?4-?(4-?pyridinyl)?-?1H-?pyrazol-?3-?yl]?phenoxy]?methyl]?- Request for quotationCAS: 1292799-56-4
Tel: 400-968-2212
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Product Name: Quinoline, 2-?[[4-?[1-?(methyl-?11C)?-?4-?(4-?pyridinyl)?-?1H-?pyrazol-?3-?yl]?phenoxy]?methyl]?- Visit Supplier Webpage Request for quotationCAS: 1292799-56-4
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