An orally bioavailable positive allosteric modulator of mGluR4 (EC50 = 1 µM); has a greater than 30-fold selectivity for mGluR4 over mGluR5 in vitro; has no activity at concentrations up to 10 µM at A2A

TCN 238 – 25 mg

Brand:
Cayman
CAS:
125404-04-8
Storage:
-20
UN-No:
Non-Hazardous - /

TCN 238 is an orally bioavailable positive allosteric modulator of the metabotropic glutamate receptor 4 (mGluR4; EC50 = 1 µM).{40126} It has a greater than 30-fold selectivity for mGluR4 over mGluR5 using human recombinant receptors in CHO-K1 cells. It has no activity at the adenosine A2A, serotonin 5-HT1A, or α2A-adrenergic receptors at concentrations up to 10 µM. In a haloperidol-induced catalepsy rat model of Parkinson’s disease, it dose-dependently reduces catalepsy with an ED50 of approximately 1 mg/kg. TCN 238 administration in rats leads to downregulation of the mGluR4 gene, GRM4, in the hippocampus and the gene for the GABAA receptor α subunit, GABRA1, in the frontal cortex without affecting hippocampal-dependent memory.{40127}  

 

Available on backorder

Add to quotes
SKU: 11994 - 25 mg Category:

Description

An orally bioavailable positive allosteric modulator of mGluR4 (EC50 = 1 µM); has a greater than 30-fold selectivity for mGluR4 over mGluR5 in vitro; has no activity at concentrations up to 10 µM at A2A, 5-HT1A, or α2A-adrenergic receptors; reduces catalepsy in a haloperidol-induced catalepsy rat model of Parkinson’s disease (ED50 = ~1 mg/kg); leads to downregulation of GRM4 and GABRA1 in rat brain without affecting hippocampal-dependent memory

Formal name: (E)-4-(2-phenylethenyl)-2-pyrimidinamine

Synonyms: 

Molecular weight: 197.2

CAS: 125404-04-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Allosteric Modulators||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease

Related products

  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 50 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 - 50 mg

    Available on backorder

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

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 10 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 - 10 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
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 50 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 50 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page