Fasiglifam hemihydrate
Based on 17 publication(s) in Google Scholar
Fasiglifam (TAK-875) hemihydrate is a potent, selective and orally active GPR40 agonist with EC50 of 72 nM. Fasiglifam enhances glucose-dependent insulin secretion and improves hyperglycemia in type 2 diabetic rats. Fasiglifam can induce liver injury.
For research use only. We do not sell to patients.
- CAS No.: 1374598-80-7
- Formula: C29H33O7.5S
- Molecular Weight:533.63
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) Fasiglifam hemihydrate
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- J Allergy Clin Immunol. 2018 Aug;142(2):470-484.e12. [Abstract]
- Phytomedicine. 2025 May:140:156618. [Abstract]
- Proc Natl Acad Sci U S A. 2023 May 30;120(22):e2219569120. [Abstract]
- Eur J Med Chem. 2022 Feb 5:229:114061. [Abstract]
- Biochem Pharmacol. 2024 Jan:219:115957. [Abstract]
- Food Funct. 2024 Apr 22;15(8):4627-4641. [Abstract]
- RSC Adv. 2019 May 15;9(26):15073-15083. [Abstract]
- Cell Regen. 2023 Mar 3;12(1):6. [Abstract]
- Chem Biol Interact. 2018 Dec 25:296:185-197. [Abstract]
- J Cell Physiol. 2022 Sep;237(9):3651-3660. [Abstract]
- Bioorg Med Chem. 2022 Feb 15:56:116615. [Abstract]
- Animals (Basel). 2025 Nov 26;15(23):3418. [Abstract]
- J Cell Biochem. 2017 May;118(5):1249-1261. [Abstract]
- PLoS One. 2018 Jul 11;13(7):e0200449. [Abstract]
- Biomed Chromatogr. 2020 Sep;34(9):e4870. [Abstract]
- Biomed Pharmacother. 2023 May:161:114509. [Abstract]
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Biological Activity
EC50: 72 nM (GPR40)[1]
Chemical Information
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CAS No. 1374598-80-7
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Molecular Weight 533.63
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Formula C29H33O7.5S
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SMILES
CC1=C(C(C)=CC(OCCCS(C)(=O)=O)=C1)C2=CC(COC3=CC=C4[C@@H](COC4=C3)CC(O)=O)=CC=C2.[0.5H2O]
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Synonyms
TAK-875 hemihydrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (17)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
J Allergy Clin Immunol
The 17,18-epoxyeicosatetraenoic acid-G protein-coupled receptor 40 axis ameliorates contact hypersensitivity by inhibiting neutrophil mobility in mice and cynomolgus macaques. [Abstract]2018 Aug;142(2):470-484.e12. PMID: 29288079 -
Phytomedicine
2025 May:140:156618. PMID: 40085989 -
Proc Natl Acad Sci U S A
2023 May 30;120(22):e2219569120. PMID: 37216523
Fasiglifam hemihydrate purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2023 May 30;120(22):e2219569120. [Abstract]
Stimulation of Gq by FFAR1 in response to TAK-875 in the presence of increasing concentrations of DHA or γLA.
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Eur J Med Chem
Discovery of new and highly effective quadruple FFA1 and PPARα/γ/δ agonists as potential anti-fatty liver agents. [Abstract]2022 Feb 5:229:114061. PMID: 34954593 -
Biochem Pharmacol
2024 Jan:219:115957. PMID: 38049007 -
Food Funct
trans-Palmitoleic acid promotes adipose thermogenesis to reduce obesity via hypothalamic FFAR1 signaling. [Abstract]2024 Apr 22;15(8):4627-4641. PMID: 38592736 -
RSC Adv
Label-free cell phenotypic study of FFA4 and FFA1 and discovery of novel agonists of FFA4 from natural products. [Abstract]2019 May 15;9(26):15073-15083. PMID: 35516320 -
Cell Regen
Modeling drug-induced liver injury and screening for anti-hepatofibrotic compounds using human PSC-derived organoids. [Abstract]2023 Mar 3;12(1):6. PMID: 36864321 -
Chem Biol Interact
Comparative hepatic transcriptome analyses revealed possible pathogenic mechanisms of fasiglifam (TAK-875)-induced acute liver injury in mice. [Abstract]2018 Dec 25:296:185-197. PMID: 30243991 -
J Cell Physiol
The role of free fatty acid receptor pathways in a selective regulation of TRPA1 and TRPV1 by resolvins in primary sensory neurons. [Abstract]2022 Sep;237(9):3651-3660. PMID: 35802479 -
Bioorg Med Chem
Design, synthesis, and biological evaluation of novel dual FFA1 and PPARδ agonists possessing phenoxyacetic acid scaffold. [Abstract]2022 Feb 15:56:116615. PMID: 35051813 -
Animals (Basel)
Divergent Regulation of Mammary Lipogenesis by trans-10, cis-12 and cis-9, trans-11 CLA Isomers Is Determined by Receptor-Specific Signaling. [Abstract]2025 Nov 26;15(23):3418. PMID: 41375476 -
J Cell Biochem
Free Fatty Acids Induce Autophagy and LOX-1 Upregulation in Cultured Aortic Vascular Smooth Muscle Cells. [Abstract]2017 May;118(5):1249-1261. PMID: 28072480
Fasiglifam hemihydrate purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2017 May;118(5):1249-1261. [Abstract]
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
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PLoS One
Anthocyanins from purple corn activate free fatty acid-receptor 1 and glucokinase enhancing in vitro insulin secretion and hepatic glucose uptake. [Abstract]2018 Jul 11;13(7):e0200449. PMID: 29995924
Fasiglifam hemihydrate purchased from MedChemExpress. Usage Cited in: PLoS One. 2018 Jul 11;13(7):e0200449. [Abstract]
TAK-875 increases (p<0.05) the membrane expression of FFAR1 compared to the untreated control by 97%.
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Biomed Chromatogr
Simultaneous determination of TUG-891 and its metabolites in rat plasma using LC-HRMS with application to preclinical pharmacokinetic study. [Abstract]2020 Sep;34(9):e4870. PMID: 32346871 -
Biomed Pharmacother
2023 May:161:114509. PMID: 37002580
Fasiglifam hemihydrate purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2023 May:161:114509. [Abstract]
Fasiglifam (0.03%; 100 μL; 14 d) promoted the telogen-anagen transition, which was demonstrated by an increased hair weight and an increased number of anagen hair follicles of C3H/HeN mice.
Fasiglifam hemihydrate purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2023 May:161:114509. [Abstract]
Fasiglifam (0.03%; 100 μL; 14 d) increased the angiogenesis around the hair follicle of C3H/HeN mice.
Fasiglifam hemihydrate purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2023 May:161:114509. [Abstract]
Fasiglifam (0.1 μM; 2 d) promoted the growth of mouse vibrissae in the mouse vibrissae organ culture model.
Fasiglifam hemihydrate purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2023 May:161:114509. [Abstract]
Fasiglifam (0.1 μM) increased the migration of hORS cells.
Purity & Documentation
References
[1]. Tsujihata Y,et al. TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats.J Pharmacol Exp [Content Brief]
[3]. Nagatake T, et al. 17,18-EpETE-GPR40 axis ameliorates contact hypersensitivity by inhibiting neutrophil mobility in mice and cynomolgus macaques. J Allergy Clin Immunol. 2017 Dec 26. pii: S0091-6749(17)32949-4. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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