PF 05180999
Modify Date: 2025-08-20 19:21:04
PF 05180999 structure
|
Common Name | PF 05180999 | ||
|---|---|---|---|---|
| CAS Number | 1394033-54-5 | Molecular Weight | 414.387 | |
| Density | 1.6±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C19H17F3N8 | Melting Point | N/A | |
| MSDS | USA | Flash Point | N/A | |
| Symbol |
GHS06 |
Signal Word | Danger | |
Use of PF 05180999PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC50 of 1.6 nM. |
| Name | PF-05180999 |
|---|---|
| Synonym | More Synonyms |
| Description | PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC50 of 1.6 nM. |
|---|---|
| Related Catalog | |
| Target |
PDE2A:1.6 nM (IC50) PDE10A1:2.03 μM (IC50) PDE11A4:26.969 μM (IC50) PDE7B:50.09 μM (IC50) |
| In Vitro | PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC50 of 1.6 nM. PF-05180999 binds to the rat, dog and monkey PDE2A, with Kis of 4.2, 8.4, and 5.5 nM and IC50s of 2.6, 5.2, and 3.4 nM, respectively. PF-05180999 shows weak activity against PDE, with IC50s of 2.03 μM (PDE10A1), 26.969 μM (PDE7B), 50.09 μM (PDE11A4), and >56.25 μM (PDE1B1, PDE3A1, PDE4D3, PDE5A1, PDE6 (bovine), PDE8B, PDE9A1), respectively. PF-05180999 is also a weak inducer of CYP3A4, and with no direct inhibition of human recombinant cytochrome P450 (CYP) enzymes (1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A) and no induction of CYP1A2[1]. |
| In Vivo | PF-05180999 (Compound 30; 0.032-0.32 mg/kg mg/kg, s.c.) dramatically reduces the working memory errors produced by ketamine in a working memory radial arm maze (RAM) model in rats. PF-05180999 causes acute and exposure-dependent elevation in the accumulation of cGMP bulk levels in the cortex, striatum, and hippocampus, but with no changes in cAMP and the associated downstream phospho-cAMP response element-binding protein (p-CREB) in mice[1]. |
| Animal Admin | Rats[1] Male Sprague-Dawley rats (weighing 250-320 g) under urethane anesthesia at 1.5 g/kg intraperitoneal (ip) are placed in a stereotaxic frame, where craniotomies are performed above the region of the medial prefrontal cortex (mPFC) and ipsilateral (CA)1/subiculum. Body temperature of the rat is maintained at 37°C with an electrical heating pad. The femoral vein is cannulated for administration of test drugs (PF-05180999, etc.). After the conclusion of the experiments animals are euthanized with an iv bolus of urethane[1]. |
| References |
| Density | 1.6±0.1 g/cm3 |
|---|---|
| Molecular Formula | C19H17F3N8 |
| Molecular Weight | 414.387 |
| Exact Mass | 414.152832 |
| LogP | 0.28 |
| Index of Refraction | 1.720 |
| Storage condition | 2-8℃ |
| Symbol |
GHS06 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H301-H315-H319-H335 |
| Precautionary Statements | P301 + P310 + P330-P305 + P351 + P338 |
| RIDADR | UN 2811 6.1 / PGIII |
| 4-(1-Azetidinyl)-7-methyl-5-{1-methyl-5-[5-(trifluoromethyl)-2-pyridinyl]-1H-pyrazol-4-yl}imidazo[5,1-f][1,2,4]triazine |
| 5L84K4IEN9 |
| Imidazo[5,1-f][1,2,4]triazine, 4-(1-azetidinyl)-7-methyl-5-[1-methyl-5-[5-(trifluoromethyl)-2-pyridinyl]-1H-pyrazol-4-yl]- |