A TSPO agonist (IC50 = 0.28 nM in a radioligand binding assay); selective for TSPO over CBR and GABAA receptors in rat whole brain membranes

DAA1106 – 1 mg

Brand:
Cayman
CAS:
220551-92-8
Storage:
-20
UN-No:
Non-Hazardous - /

DAA1106 is an agonist of the 18 kDa translocator protein TSPO, which was previously known as the peripheral benzodiazepine receptor (PBR), that has an IC50 value of 0.28 nM in a radioligand binding assay.{41208} It is selective for TSPO over central benzodiazepine receptors (CBRs) and GABAA receptors in rat whole brain membranes, as well as a panel of 54 ion channels, uptake/transporters, and secondary messenger receptors at concentrations greater than 10 µM. DAA1106 increases mitochondrial prognenolone formation in rat brain homogenates, which indirectly potentiates GABAA receptor signaling. DAA1106 (1-10 mg/kg) increases the time mice spend in the light area of the light/dark exploration and the time rats spend in open arms of the elevated plus maze in a dose-dependent manner, suggesting a decrease in anxiety-like behavior. Various radiolabeled versions of DAA1106 have been synthesized to study the distribution of PBRs in neurological disease models using positron emission tomography (PET).{41209,41210}  

 

Available on backorder

Add to quotes
SKU: 23454 - 1 mg Category:

Description

A TSPO agonist (IC50 = 0.28 nM in a radioligand binding assay); selective for TSPO over CBR and GABAA receptors in rat whole brain membranes, as well as a panel of 54 ion channels, uptake/transporters, and secondary messenger receptors at concentrations greater than 10 µM; increases mitochondrial prognenolone formation in rat brain homogenates, which indirectly potentiates GABAA receptor signaling; increases the time mice spend in the light area of the light/dark exploration and the time rats spend in open arms of the elevated plus maze in a dose-dependent manner, suggesting a decrease in anxiety-like behavior; radiolabeled versions have been synthesized to study the distribution of PBRs in neurological disease models using PET

Formal name: N-[(2,5-dimethoxyphenyl)methyl]-N-(5-fluoro-2-phenoxyphenyl)-acetamide

Synonyms: 

Molecular weight: 395.4

CAS: 220551-92-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Activators||Research Area|Neuroscience|Behavioral Neuroscience|Anxiety

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 – 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
  • 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 – 1 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 - 1 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 – 10 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 - 10 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page