509104 AdipoR Agonist, AdipoRon - Calbiochem

509104
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₇H₂₈N₂O₃

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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable benzylpiperidinyl-acetamide compound that acts as an adiponectin receptor agonist (KD = 1.8 µM and 3.1 µM, respectively, toward human AdipoR1 and AdipoR2; KD = 6.9 µM and 6.0 µM, respectively, toward murine AdipoR1 and AdipoR2), effectively stimulating AMPK α-subunit Thr172 phosphorylation in murine myoblast C2C12 cultures (1 to 50 µM; 5 min) in vitro and in skeletal muscle & liver tissues in mice (50 mg/kg i.v.) in vivo. Oral administration in either db/db or high-fat diet-induced wt obese mice (50 mg/kg/d for 10 d to 2 wks) is reported to increase insulin sensitivity and glucose tolerance via activation of AdipoR1-mediated AMPK pathway in muscle & liver, as well as AdipoR2-mediated PPAR-α pathway in liver in vivo, resulting in enhanced exercise endurance and prolonged lifespan.
      Catalogue Number509104
      Brand Family Calbiochem®
      Synonyms2-(4-Benzoylphenoxy)-N-(1-benzylpiperidin-4-yl)acetamide, Adiponectin Receptor Agonist
      References
      ReferencesOkada-Iwabu, M., et al. 2013. Nature 503, 493.
      Product Information
      FormTan solid
      Hill FormulaC₂₇H₂₈N₂O₃
      Chemical formulaC₂₇H₂₈N₂O₃
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetAdipoR1 and AdipoR2
      Primary Target K<sub>i</sub>1.8 and 3.1 µ
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      AdipoR Agonist, AdipoRon - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Okada-Iwabu, M., et al. 2013. Nature 503, 493.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision21-February-2014 JSW
      Synonyms2-(4-Benzoylphenoxy)-N-(1-benzylpiperidin-4-yl)acetamide, Adiponectin Receptor Agonist
      DescriptionA cell-permeable benzylpiperidinyl-acetamide compound that acts as an adiponectin receptor agonist (KD = 1.8 µM and 3.1 µM, respectively, in binding studies using human AdipoR1 or AdipoR2; KD = 6.9 µM and 6.0 µM, respectively, using hepatocytes from AdipoR1+/+AdipoR2-/- or AdipoR1-/-AdipoR2+/+ mice), effectively stimulating AMPK α-subunit Thr172 phosphorylation in murine myoblast C2C12 cultures (1 to 50 µM; 5 min) in vitro and in skeletal muscle and liver tissues in mice (50 mg/kg i.v.) in vivo without affecting mitochondrial complex I activity. Oral administration (Plasma Cmax/Tmax post 50 mg/kg oral dosing = 11.8 µM/40 min) in either db/db or high-fat diet-induced wt obese mice (for 10 d to 2 wks) is reported to increase insulin sensitivity and glucose tolerance via activation of AdipoR1-mediated AMPK pathway in muscle and liver, as well as AdipoR2-mediated PPAR-α pathway in liver, resulting in enhanced exercise endurance and prolonged lifespan. In addition to muscle mitochondrial biogenesis enhancement and liver gluconeogenesis inhibition, reduced oxidative stress in calf muscle, liver, and white adipose tissue (WAT), as well as reduced expressions of pro-inflammatory cytokines in liver and WAT are also observed in AdipoRon-treated obese mice in vivo.
      FormTan solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₇H₂₈N₂O₃
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesOkada-Iwabu, M., et al. 2013. Nature 503, 493.