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Firuglipel

CAS No. 1371591-51-3

Firuglipel( DS-8500 | DS8500a )

Catalog No. M11532 CAS No. 1371591-51-3

Firuglipel (DS-8500, DS8500a) is a novel potent, selective, orally available GPR119 agonist with EC50 of 51.5 nM in human GPR119-expressing CHO-K1 cells.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Firuglipel
  • Note
    Research use only, not for human use.
  • Brief Description
    Firuglipel (DS-8500, DS8500a) is a novel potent, selective, orally available GPR119 agonist with EC50 of 51.5 nM in human GPR119-expressing CHO-K1 cells.
  • Description
    Firuglipel (DS-8500, DS8500a) is a novel potent, selective, orally available GPR119 agonist with EC50 of 51.5 nM in human GPR119-expressing CHO-K1 cells, displays no significant effect on 66 receptors, channels, or transporters; enhances glucose-stimulated insulin secretion in Sprague-Dawley rats and promotes GLP-1 secretion in Zucker fatty rats, preserved β cell function and prevented increases in glycohemoglobin concentrations in rodent models of type 2 diabetes.Diabetes Phase 2 Clinical.
  • In Vitro
    Firuglipel (DS-8500a) increases intracellular cAMP in a concentration-dependent manner in human, rat, and mouse GPR119-expressing Chinese hamster ovary (CHO)-K1 cells, with EC50 values of 51.5, 98.4, and 108.1 nM, respectively. DS-8500a has no effect on intracellular cAMP in pcDNA3.1/CHO-K1 cells.
  • In Vivo
    Firuglipel (DS-8500a) (1-30 mg/kg) upregulates glucagon-like peptide-1 and enhances glucose-dependent insulin secretion and improves glucose homeostasis in type 2 diabetic rats.
  • Synonyms
    DS-8500 | DS8500a
  • Pathway
    GPCR/G Protein
  • Target
    GPR119
  • Recptor
    GPR119
  • Research Area
    Metabolic Disease
  • Indication
    Diabetes

Chemical Information

  • CAS Number
    1371591-51-3
  • Formula Weight
    467.497
  • Molecular Formula
    C25H26FN3O5
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    O=C(N[C@@H](C)CO)C1=CC=C(C2=NOC([C@@H](OC3=CC=C(C(C4CC4)=O)C=C3)CC)=N2)C=C1F
  • Chemical Name
    4-(5-{(1R)-1-[4-(cyclopropanecarbonyl)phenoxy]propyl}-1,2,4-oxadiazol-3-yl)-2-fluoro-N-[(2R)-1-hydroxypropan-2-yl]benzamide

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Patent WO2012050151. 2.?Inagaki N, et al. BMJ Open Diabetes Res Care. 2017 Sep 29;5(1):e000424. 3.?Terauchi Y, et al. J Diabetes Investig. 2018 Apr 1. doi: 10.1111/jdi.12846. 4.?Makino C, et al. Xenobiotica. 2018 Aug 20:1-33. doi: 10.1080/00498254.2018.1514545.
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