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Fasiglifam

CAS No. 1000413-72-8

Fasiglifam( Fasiglifam | TAK 875 | TAK875 )

Catalog No. M10006 CAS No. 1000413-72-8

A potent, selective, orally bioavailable GPR40 (FFA1) agonist with EC50 of 14 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Fasiglifam
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, selective, orally bioavailable GPR40 (FFA1) agonist with EC50 of 14 nM.
  • Description
    A potent, selective, orally bioavailable GPR40 (FFA1) agonist with EC50 of 14 nM; exhibited excellent agonist potency selectivity over other FFA receptors (GPR41, GPR43, and GPR120, EC50s>10 uM); shows potent plasma glucose-lowering action and insulinotropic action in vivo.Diabetes Phase 3 Discontinued(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. 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.(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 .
  • 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. 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.
  • 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 .
  • Synonyms
    Fasiglifam | TAK 875 | TAK875
  • Pathway
    GPCR/G Protein
  • Target
    FFAR
  • Recptor
    GPR40(FFA1)
  • Research Area
    Metabolic Disease
  • Indication
    Diabetes

Chemical Information

  • CAS Number
    1000413-72-8
  • Formula Weight
    524.6252
  • Molecular Formula
    C29H32O7S
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 128 mg/mL
  • SMILES
    CC1=C(C2=CC(COC3=CC=C([C@H](CC(O)=O)CO4)C4=C3)=CC=C2)C(C)=CC(OCCCS(C)(=O)=O)=C1
  • Chemical Name
    3-Benzofuranacetic acid, 6-[[2',6'-dimethyl-4'-[3-(methylsulfonyl)propoxy][1,1'-biphenyl]-3-yl]methoxy]-2,3-dihydro-, (3S)-

Shipping & Storage Information

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

Reference

1. Negoro N, et al. ACS Med Chem Lett. 2010 Jun 18;1(6):290-4. 2. Tsujihata Y, et al. J Pharmacol Exp Ther. 2011 Oct;339(1):228-37. 3. Yashiro H,J Pharmacol Exp Ther. 2012 Feb;340(2):483-9. 4. Ito R, et al. Br J Pharmacol. 2013 Oct;170(3):568-80.
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  • Fasiglifam

    A potent, selective, orally bioavailable GPR40 (FFA1) agonist with EC50 of 14 nM.

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