533469 GPR120 Agonist IV, cpdA - CAS 1599477-75-4 - Calbiochem

533469
Price could not be retrieved
Minimum Quantity needs to be mulitiple of
Upon Order Completion More Information
You Saved ()
 
Request Pricing
Limited AvailabilityLimited Availability
Stocked 
Discontinued
Limited Quantities Available
Available
    Remaining : Will advise
      Remaining : Will advise
      Will advise
      Contact Customer Service
      Contact Customer Service
      View Pricing & Availability

      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₉H₂₃ClF₃NO₃ 1599477-75-4

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.33469.0001
      Retrieving availability...
      Limited AvailabilityLimited Availability
      Stocked 
      Discontinued
      Limited Quantities Available
      Available
        Remaining : Will advise
          Remaining : Will advise
          Will advise
          Contact Customer Service
          Contact Customer Service

          Glass bottle 10 mg
          Retrieving price...
          Price could not be retrieved
          Minimum Quantity needs to be mulitiple of
          Upon Order Completion More Information
          You Saved ()
           
          Request Pricing
          Description
          OverviewA cell-permeable, orally active, non-toxic, azaspiroundecanyl acetic acid based compound that acts as a highly potent, selective and reversible activator of GPR120 in murine and human cells (EC50 = 350 nM for β-arrestin 2 recruitment). Induces concentration-dependent increase in inositol-1,4,5-triphosphate (IP3) production in GRP120 expressing cells. Exhibits about 50-fold higher sensitivity for GRP120 than docosahexaenoic acid, however, it displays very poor affinity towards GRP40. Effectively reduces hepatic steatosis and improves glucose tolerance, hyperinsulinemia, and insulin sensitivity in obese mice fed high fat diet. Strongly inhibits LPS-induced phosphorylation of TAK1, IKKβ & JNK and reduces IκB degradation in macrophages.

          Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
          Catalogue Number533469
          Brand Family Calbiochem®
          Synonyms2-(3-(2-Chloro-5-(trifluoromethoxy)phenyl)-3-azaspiro[5.5]undecan-9-yl)acetic acid
          References
          ReferencesOh, D.Y., et al. 2014. Nat. Med. 8, 942.
          Product Information
          CAS number1599477-75-4
          FormOff-white solid
          Hill FormulaC₁₉H₂₃ClF₃NO₃
          Chemical formulaC₁₉H₂₃ClF₃NO₃
          ReversibleY
          Applications
          Biological Information
          Primary TargetGPR120
          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 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          GPR120 Agonist IV, cpdA - CAS 1599477-75-4 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Oh, D.Y., et al. 2014. Nat. Med. 8, 942.
          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.

          Revision23-July-2016 JSW
          Synonyms2-(3-(2-Chloro-5-(trifluoromethoxy)phenyl)-3-azaspiro[5.5]undecan-9-yl)acetic acid
          DescriptionA cell-permeable azaspiroundecanyl acetic acid compound that acts as a selective Gpr120 (FFAR4) agonist toward both human and murine species (EC50 = 60 nM/IP3 production and 350 nM/β-Arrestin-2 recruitment using cells expressing human or murine Gpr120), while being ineffective toward Gpr40 and is about 100-fold more effective than docosahexaenoic acid/DHA in stimulating serum response element/SRE promoter-mediated reporter transcription in mGPR120-expressing HEK 293. Selectively suppresses (10 µM) chemotaxis toward adipocyte-conditioned medium and LPS-induced inflammatory responses in primary macrophages derived from wt, but not Gpr120-knockout, mice in vitro, including IκB degradation as well as phosphorylations of Tak1, Ikk-β, and JNK, and is efficacious in improving glucose tolerance & insulin sensitivity in vivo among wt, but not Gpr120-knockout, mice on high-fat diet (HFD) when supplemented (30 mg/kg) in the diet for the last 5 wks of a 20-wk HFD period without affecting animal body weight, resulting in decreased hyperinsulinemia, hepatic steatosis, adipose tissue macrophage (ATM) infiltration and inflammation. Unlike the Gpr40/Gpr120 dual agonist DHA, this compound does not stimulate Gpr40-mediated insulin secretion from MIN6 β cell line or ehances Glucose-stimulated insulin secretion (GSIS) from β cells in cultured islets from wt or Gpr120-knockout mice.
          FormOff-white solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number1599477-75-4
          Chemical formulaC₁₉H₂₃ClF₃NO₃
          Purity≥97% by HPLC
          SolubilityDMSO (50 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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesOh, D.Y., et al. 2014. Nat. Med. 8, 942.