A potent inhibitor of PDE10A (IC50 = 1.26 nM for the human recombinant enzyme); selective for PDE10A over other PDEs with IC50 values ranging from 1.7 to >10 μM; increases cAMP and cGMP production as well as phosphorylation of CREB and GluR1 in mouse striatum in a dose-dependent manner; reduces apomorphine-induced climbing behavior in mice (ID50 = 0.375 mg/kg) and disrupts the conditioned avoidance response in mice and rats (ID50s = 0.441 and 1.079 mg/kg

PF-2545920 – 5 mg

Brand:
Cayman
CAS:
898562-94-2
Storage:
-20
UN-No:
Non-Hazardous - /

PF-2545920 is a potent inhibitor of phosphodiesterase 10A (PDE10A; IC50 = 1.26 nM for the human recombinant enzyme).{38516} It is selective for PDE10A over other PDEs with IC50 values ranging from 1.7 to >10 μM. In vivo, PF-2545920 (0.1-3 mg/kg, i.p.) increases cAMP and cGMP production as well as phosphorylation of CREB and GluR1 in mouse striatum in a dose-dependent manner. It reduces climbing behavior induced by apomorphine (Item No. 16094) in mice (ID50 = 0.375 mg/kg) and disrupts the conditioned avoidance response in mice and rats (ID50s = 0.441 and 1.079 mg/kg, respectively). PF-2545920 reverses deficits in prepulse inhibition and social odor recognition induced by (+)-MK-801 (Item No. 10009019) in rats. Formulations containing PF-2545920 are under clinical investigation for the treatment of schizophrenia and Huntington’s disease.  

 

Available on backorder

Add to quotes
SKU: - Category:

Description

A potent inhibitor of PDE10A (IC50 = 1.26 nM for the human recombinant enzyme); selective for PDE10A over other PDEs with IC50 values ranging from 1.7 to >10 μM; increases cAMP and cGMP production as well as phosphorylation of CREB and GluR1 in mouse striatum in a dose-dependent manner; reduces apomorphine-induced climbing behavior in mice (ID50 = 0.375 mg/kg) and disrupts the conditioned avoidance response in mice and rats (ID50s = 0.441 and 1.079 mg/kg, respectively); reverses (+)-MK-801-induced deficits in prepulse inhibition and social odor recognition in rats,

Formal name: 2-[[4-[1-methyl-4-(4-pyridinyl)-1H-pyrazol-3-yl]phenoxy]methyl]-quinoline

Synonyms: 

Molecular weight: 392.5

CAS: 898562-94-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phosphodiesterases||Research Area|Neuroscience|Behavioral Neuroscience|Schizophrenia & Psychosis||Research Area|Neuroscience|Neurodegenerative Disorders|Huntington’s Disease

Related products

  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 25 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 25 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 100 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 100 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 10 mg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 10 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 50 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 50 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page