An agonist of nicotinic AChRs; selective for α4β2 or α7 subunit-containing nicotinic AChRs (Kis = 0.7 and 10.9 nM in isolated rat cortex and isolated rat hippocampus

RJR 2429 (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
1021418-53-0
Storage:
-20
UN-No:
Non-Hazardous - /

RJR 2429 is a nicotinic acetylcholine receptor (AChR) agonist.{49443} It is selective for α4β2 or α7 subunit-containing nicotinic AChRs (Kis = 0.7 and 10.9 nM in isolated rat cortex and isolated rat hippocampus, respectively) over α1βɣδ subunit-containing nicotinic AChRs (EC50 = 1,000 nM in PC12 cells). RJR 2429 induces dopamine release from isolated rat striatal synaptosomes (EC50 = 2.4 nM) and increases nicotine-induced elevations in epinephrine and norepinephrine levels in isolated rat adrenal gland when used at a concentration of 100 µM.{49444},{49446} It inhibits nicotine-induced ion flux in isolated rat thalamic synaptosomes (IC50 = 154 nM).{49444}  

 

Available on backorder

Add to quotes
SKU: 29745 - 10 mg Category:

Description

An agonist of nicotinic AChRs; selective for α4β2 or α7 subunit-containing nicotinic AChRs (Kis = 0.7 and 10.9 nM in isolated rat cortex and isolated rat hippocampus, respectively) over α1βɣδ subunit-containing nicotinic AChRs (EC50 = 1,000 nM in PC12 cells); induces dopamine release from isolated rat striatal synaptosomes (EC50 = 2.4 nM) and increases nicotine-induced elevations in epinephrine and norepinephrine levels in isolated rat adrenal gland at 100 µM; inhibits nicotine-induced ion flux in isolated rat thalamic synaptosomes (IC50 = 154 nM)

Formal name: 2-(3-pyridinyl)-1-azabicyclo[2.2.2]octane, dihydrochloride

Synonyms: 

Molecular weight: 261.2

CAS: 1021418-53-0

Purity: ≥98%

Formulation: A solid

Related products

  • 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 – 100 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 - 100 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 – 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
  • 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
  • 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