A potent and selective agonist of M1 receptors (EC50 = 0.2 mM compared to >10 mM for M2-M5); induces concentration-dependent increases in Ca2+ mobilization and ERK1/2 phosphorylation in hM1 CHO cells (EC50s = 0.89 and 10 mM

VU0364572 (trifluoroacetate salt) – 25 mg

Brand:
Cayman
CAS:
1240514-89-9
Storage:
-20
UN-No:
Non-Hazardous - /

VU0364572 is a potent and selective agonist of the muscarinic acetylcholine receptor 1 (M1; EC50 = 0.2 mM compared to >10 mM for M2-M5).{37299} It induces concentration-dependent increases in Ca2+ mobilization and ERK1/2 phosphorylation in CHO cells transfected with the human M1 receptor (EC50s = 0.89 and 10 mM, respectively) with no effect on β-arrestin recruitment. VU0364572 also improves hippocampal-dependent spatial learning and localization abilities and acquistion of contextual fear learning but cannot reverse amphetamine-induced hyperlocomotion in rats. This suggests therapeutic potential of VU0364572 for the treatment of Alzheimer’s disease but not psychosis.{37300}  

 

Available on backorder

Add to quotes
SKU: 20466 - Category:

Description

A potent and selective agonist of M1 receptors (EC50 = 0.2 mM compared to >10 mM for M2-M5); induces concentration-dependent increases in Ca2+ mobilization and ERK1/2 phosphorylation in hM1 CHO cells (EC50s = 0.89 and 10 mM, respectively); improves hippocampal-dependent spatial learning and localization abilities and acquistion of contextual fear learning but cannot reverse amphetamine-induced hyperlocamotion in rats

Formal name: (3R)-3-[(2-methylbenzoyl)amino]-[1,4′-bipiperidine]-1′-carboxylic acid, ethyl ester, 2,2,2-trifluoroacetate

Synonyms: 

Molecular weight: 487.5

CAS: 1240514-89-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory

Related products

  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 1 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 1 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 25 mg

    1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}  

     

    Brand:
    Cayman
    SKU:10009473 - 25 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 25 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 25 mg

    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 – 500 µg

    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 - 500 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page