1. GPCR/G Protein
  2. GPR40
  3. Fasiglifam

Fasiglifam (Synonyms: TAK-875)

Cat. No.: HY-10480 Purity: 98.94%
Handling Instructions

Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM.

For research use only. We do not sell to patients.

Fasiglifam Chemical Structure

Fasiglifam Chemical Structure

CAS No. : 1000413-72-8

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10 mM * 1 mL in DMSO USD 139 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Fasiglifam purchased from MCE. Usage Cited in: J Cell Biochem. 2017 May;118(5):1249-1261.

    Free fatty acid receptor 1 (FFAR1) agonist induces LOX-1 upregulation in cultured vascular smooth muscle cells (VSMCs). Cultured VSMCs are treated with synthetic agonists for either FFAR1 (TAK-875) or FFAR4 (TUG-891) at indicated doses for 24 hours. Both FFAR1 and FFAR4 are known responsible for long chain fatty acids. 0.1% DMSO is used as solvent control (SC). Western blotting detection indicates that treatment with agonistic action of FFAR1, but not FFAR4, remarkably upregulated LOX-1 expressi

    Fasiglifam purchased from MCE. Usage Cited in: PLoS One. 2018 Jul 11;13(7):e0200449.

    TAK-875 increases (p<0.05) the membrane expression of FFAR1 compared to the untreated control by 97%.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM.

    IC50 & Target

    EC50: 72 nM (GPR40)

    In Vitro

    Fasiglifam (TAK-875) (0.01-10 μM) produces a concentration-dependent increase in intracellular IP production in CHO-hGPR40, with EC50 of 0.072 μM. Fasiglifam (TAK-875) (0.1-10 μM) dose-dependently augments intracellular IP production in CHO cells[1]. Fasiglifam (TAK-875) (3-30 μM) concentration-dependently augments [Ca2+]i. In the presence of 10 mM glucose, TAK-875 (0.001-10 μM) dose-dependently stimulats insulin secretion from INS-1 833/15 cells[2].

    In Vivo

    Fasiglifam (TAK-875) (10 mg/kg, p.o.) increases plasma insulin levels in ZDF rats. Fasiglifam (TAK-875) (30 mg/kg, p.o.) improves fasting hyperglycemia without affecting fasting normoglycemia. Fasiglifam (TAK-875) at 30 mg/kg, which is a 3- to 10-fold higher dose compared with the dose that improved glucose tolerance in diabetic rats, does not alter fasting glucose levels in SD rats with normal glucose homeostasis. Likewise, Fasiglifam (TAK-875) does not significantly alter insulin secretion in SD rats with normal fasting glucose levels [1].

    Clinical Trial
    Molecular Weight

    524.63

    Formula

    C₂₉H₃₂O₇S

    CAS No.

    1000413-72-8

    SMILES

    CC1=C(C(C)=CC(OCCCS(C)(=O)=O)=C1)C2=CC(COC3=CC=C4[[email protected]@H](COC4=C3)CC(O)=O)=CC=C2

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 128 mg/mL (243.98 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9061 mL 9.5305 mL 19.0611 mL
    5 mM 0.3812 mL 1.9061 mL 3.8122 mL
    10 mM 0.1906 mL 0.9531 mL 1.9061 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.77 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.77 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.77 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    INS-1 832/13 cells are suspended in RPMI medium and seeded in a 96-well plate at a density of 2×104 cells/well; 1% BSA and 0.1% DMSO alone (control), palmitic acid (10, 100, and 1000 μM), oleic acid (10, 100, and 1000 μM), or Fasiglifam (TAK-875: 1, 10, and 100 μM) is added to the plate. After 72-h culture, medium is discarded, and cells are preincubated for 2 h with KRBH containing 1 mM glucose and 0.2% BSA at 37°C. After discarding of the preincubation buffer, KRBH containing 1 or 20 mM glucose and 0.2% BSA is added, and the plate is further incubated for 2 h. The insulin concentration in the supernatant is measured as described above. To measure intracellular insulin content, INS-1 832/13 cells are exposed to 1% BSA and 0.1% DMSO alone (control), palmitic acid (1000 μM), oleic acid (1000 μM), or Fasiglifam (TAK-875) (100 μM) with 1% BSA and 0.1% DMSO. After incubation, cells are washed once with phosphate-buffered saline, and acid-ethanol solution is added to each well, followed by sonication on ice. Intracellular insulin is extracted by overnight incubation at −30°C, followed by separation of supernatant by centrifugation at 12,000 rpm×5 min at 4°C.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    At 18 weeks of age, the N-STZ-1.5 rats are fasted overnight and orally given vehicle (0.5% methylcellulose) or Fasiglifam (TAK-8751, 3, and 10 mg/kg). Sixty minutes later, all animals receive an oral glucose load (1 g/kg). Blood samples are collected from the tail vein before drug administration, before glucose load (time 0), and 10, 30, 60, and 120 min after the glucose load. Plasma glucose and insulin levels are measured with an AutoAnalyzer 7080 and radioimmunoassay, respectively. To see the effects of Fasiglifam (TAK-875) on fasting normoglycemia and hyperglycemia, SD rats (8 weeks old) or ZDF and ZL rats (12 weeks old) are fasted overnight and orally given vehicle (0.5% methylcellulose), Fasiglifam (TAK-875) (10 or 30 mg/kg), nateglinide (50 mg/kg), or glibenclamide (10 mg/kg). Blood samples are collected from the tail vein before drug administration (time 0) and 0.5, 1, 2, and 3 h (SD rats) and 0.5, 1, 2, 4, and 6 h (ZDF and ZL rats) after drug administration, and plasma glucose and insulin levels are measured as described above.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 98.94%

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    Fasiglifam
    Cat. No.:
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