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GPR120-IN-1

Cat. No. M5292
GPR120-IN-1 Structure
Size Price Availability Quantity
10mg USD 210 In stock
50mg USD 660 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

In vitro: GPR120-IN-1 is fully selective for Gpr120 (logEC50=?7.62) with negligible activity towards Gpr40. GPR120-IN-1 produces concentration dependent increases in IP3 production from both human and mouse Gpr120 expressing cells. GPR120-IN-1 leads to a concentration-dependent response to recruit β-arrestin-2 in both human and mouse Gpr120 expressing cells, with EC50s of ~0.35 μM. GPR120-IN-1 strongly and comparably inhibits LPS-induced phosphorylation of Tak1, Ikkβ, and Jnk and blocked IκB degradation. In vivo: GPR120-IN-1 causes improved insulin sensitivity with increased glucose infusion rates, enhanced insulin stimulated-glucose disposal rate, along with a marked increase in the ability of insulin to suppress hepatic glucose production only in WT mice. GPR120-IN-1 treatment has beneficial effects on hepatic lipid metabolism, causing decreased hepatic steatosis, decreased liver triglycerides, and DAGs, along with reduced saturated free fatty acid conten.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Male C57Bl/6 WT or Gpr120 KO rats
Formulation 10% FBS
Dosages 30 mg / kg
Administration i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 405.84
Formula C19H23ClF3NO3
CAS Number 1599477-75-4
Purity >99%
Solubility 10mM in DMSO
Storage at -20°C
References

Biological characteristics and agonists of GPR120 (FFAR4) receptor: the present status of research.
Li A, et al. Future Med Chem. 2015;7(11):1457-68. PMID: 26230883.

A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice.
Oh DY, et al. Nat Med. 2014 Aug;20(8):942-7. PMID: 24997608.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GPR120-IN-1 supplier, GPR, inhibitors

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