An α2-AR (EC50s = 1 receptor antagonist; binds to α2A-

Efaroxan (hydrochloride) – 50 mg

Brand:
Cayman
CAS:
89197-00-2
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Efaroxan is an α2-adrenergic receptor (α2-AR; EC50s = 1 receptor antagonist.{52072} It binds to α2A-, α2B-, and α2C-ARs (Kis = 13, 38, and 1,820 nM, respectively) and selectively to I1 over I2 receptors (Kis = 52 and >10,000 nM, respectively). Efaroxan is an I3 agonist that binds to putative I3 receptors on human pancreatic islets of Langerhans and stimulates insulin secretion when used at a concentration of 100 μM.{52073} It also binds to rat RIN-5AH insulinoma cell membranes (IC50 = 32 nM) and stimulates insulin secretion when used at a concentration of 100 μM.{52074} Efaroxan (5 mg/kg) lowers basal blood glucose levels in mice.{52075} It also increases 3,4-dihydroxyphenylalanine (L-DOPA; Item No. 13248) synthesis in rat cortex and hippocampus by 77 and 57%, respectively, when administered at a dose of 10 mg/kg.{52076}  

 

Available on backorder

Add to quotes
SKU: 29008 - 50 mg Category:

Description

An α2-AR (EC50s = 1 receptor antagonist; binds to α2A-, α2B-, and α2C-ARs (Kis = 13, 38, and 1,820 nM, respectively) and selectively to I1 over I2 receptors (Kis = 52 and >10,000 nM, respectively); binds to putative I3 receptors on human pancreatic islets of Langerhans and stimulates insulin secretion at 100 μM; binds to rat RIN-5AH insulinoma cell membranes (IC50g = 32 nM) and stimulates insulin secretion at 100 μM; lowers basal blood glucose levels in mice at 5 mg/kg; increases L-DOPA synthesis in rat cortex and hippocampus by 77 and 57%, respectively at 10 mg/kg

Formal name: 2-(2-ethyl-2,3-dihydro-2-benzofuranyl)-4,5-dihydro-1H-imidazole, monohydrochloride

Synonyms:  (±)-Efaroxan|RX 821037

Molecular weight: 252.7

CAS: 89197-00-2

Purity: ≥98%

Formulation: A solid

Related products

  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 250 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 250 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 – 500 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 - 500 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 – 100 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 - 100 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 – 250 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 - 250 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page