509104 AdipoR Agonist, AdipoRon - Calbiochem

509104
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₇H₂₈N₂O₃

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.09104.0001
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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®
          SynonymsAdiponectin Receptor Agonist, 2-(4-Benzoylphenoxy)-N-(1-benzylpiperidin-4-yl)acetamide
          References
          ReferencesOkada-Iwabu, M., et al. 2013. Nature 503, 493.
          Product Information
          FormTan solid
          Hill FormulaC₂₇H₂₈N₂O₃
          Chemical formulaC₂₇H₂₈N₂O₃
          ReversibleY
          Structure formula ImageStructure formula Image
          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

          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
          SynonymsAdiponectin Receptor Agonist, 2-(4-Benzoylphenoxy)-N-(1-benzylpiperidin-4-yl)acetamide
          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.