2115022-67-6
Chemical Structure
PF-06827443
- CAS No.: 2115022-67-6
- Formula:C24H24N2O4
- Molecular Weight:404.46
IUPAC Name: 2-((3R,4S)-3-hydroxytetrahydro-2H-pyran-4-yl)-5-methyl-6-(4-(oxazol-4-yl)benzyl)isoindolin-1-one
InChIKey: RBMHKFVYRIRMOG-GOTSBHOMSA-N
SMILES: O=C1C2=CC(CC3=CC=C(C4=COC=N4)C=C3)=C(C)C=C2CN1[C@@H]5[C@H](COCC5)O
Biological Activity: PF-06827443 is an orally active M1 receptor positive allosteric modulator with an EC50 of 47 nM and a Ki of 16 nM, and a PDE11A4 inhibitor with an IC50 of 5.06 μM. PF-06827443 enhances the effects of acetylcholine. PF-06827443 crosses the blood-brain barrier, induces LTD in the prefrontal cortex, increases sEPSC frequency in layer V pyramidal cells, and increases striatal inositol monophosphate accumulation. PF-06827443 induces convulsions, impairs cognition, reduces stimulant-evoked locomotion, reverses Scopolamine (HY-N0296)-induced learning/memory deficits, and causes cholinergic adverse events and convulsions in rats and dogs. PF-06827443 can be used for research on schizophrenia and Alzheimer's disease[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
PF-06827443 | PF-06827443 is an orally active M1 receptor positive allosteric modulator with an EC50 of 47 nM and a Ki of 16 nM, and a PDE11A4 inhibitor with an IC50 of 5.06 μM. PF-06827443 enhances the effects of acetylcholine. PF-06827443 crosses the blood-brain barrier, induces LTD in the prefrontal cortex, increases sEPSC frequency in layer V pyramidal cells, and increases striatal inositol monophosphate accumulation. PF-06827443 induces convulsions, impairs cognition, reduces stimulant-evoked locomotion, reverses Scopolamine (HY-N0296)-induced learning/memory deficits, and causes cholinergic adverse events and convulsions in rats and dogs. PF-06827443 can be used for research on schizophrenia and Alzheimer's disease. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Moran SP, et al. PF-06827443 Displays Robust Allosteric Agonist and Positive Allosteric Modulator Activity in High Receptor Reserve and Native Systems. ACS chemical neuroscience. 2018 Sep 19;9(9):2218-2224.
- [2]. Rook JM, et al. A Novel M PAM VU0486846 Exerts Efficacy in Cognition Models without Displaying Agonist Activity or Cholinergic Toxicity. ACS chemical neuroscience. 2018 Sep 19;9(9):2274-2285.
- [3]. Davoren JE, et al. Design and Synthesis of γ- and δ-Lactam M Positive Allosteric Modulators (PAMs): Convulsion and Cholinergic Toxicity of an M-Selective PAM with Weak Agonist Activity. Journal of medicinal chemistry. 2017 Aug 10;60(15):6649-6663. [Content Brief]
