| Identification | Back Directory | [Name]
TAK875 | [CAS]
1000413-72-8 | [Synonyms]
CS-54
TAK875
Fasiglifam
TAK-875, >=98%
TAK-875,TAK875
TAK875 USP/EP/BP
TAK-875(Fasiglifam)
FASIGLIFAM (TAK-875)
TAK-875; TAK875; TAK 875.
(S)-2-(6-((2',6'-Dimethyl-4'-(3-(methylsulfonyl)propoxy)-[1,1'-biphenyl]-3-yl)methoxy)-2,3-dih
[(3S)-6-({3-[4-(3-methanesulfonylpropoxy)-2,6-dimethylphenyl]phenyl}methoxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid
(3S)-6-[[2',6'-Dimethyl-4'-[3-(methylsulfonyl)propoxy][1,1'-biphenyl]-3-yl]methoxy]-2,3-dihydro-3-benzofuranacetic acid
[(3S)-6-({2',6'-Dimethyl-4'-[3-(methylsulfonyl)propoxy]-3-biphenylyl}methoxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid
3-Benzofuranacetic acid, 6-[[2',6'-diMethyl-4'-[3-(Methylsulfonyl)propoxy][1,1'-biphenyl]-3-yl]Methoxy]-2,3-dihydro-, (3S)-
(S)-2-(6-((2',6'-Dimethyl-4'-(3-(methylsulfonyl)propoxy)-[1,1'-biphenyl]-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid | [Molecular Formula]
C29H32O7S | [MDL Number]
MFCD18251445 | [MOL File]
1000413-72-8.mol | [Molecular Weight]
524.625 |
| Chemical Properties | Back Directory | [Melting point ]
123-127°C | [Boiling point ]
739.1±60.0 °C(Predicted) | [density ]
1.252 | [storage temp. ]
Refrigerator | [solubility ]
Acetonitrile (Slightly), DMSO (Slightly), Methanol (Slightly) | [form ]
Solid | [pka]
4.36±0.10(Predicted) | [color ]
White to Off-White |
| Hazard Information | Back Directory | [Description]
The free fatty acid receptor 1 (FFAR1; GPR40) is highly expressed in pancreatic β-cells and activated by medium and long-chain fatty acids.1 There is evidence of a link between FFAR1 (GPR40) and the ability of fatty acids to amplify glucose-stimulated insulin secretion, making this signaling pathway a potential target for regulating diabetes, obesity, and other metabolic disorders.2,3 TAK-875 is a selective FFAR1 (GPR40) agonist (EC50 = 26 nM) that does not exhibit activity on the related FFARs FFAR2 (GPR43) or FFAR3 (GPR41).4 | [Uses]
TAK-876 is a selective G protein-coupled receptor 40 (GPR40) agonist. TAK-876 is a novel oral medication that has been developed to improve the secretion of insulin in a glucose-dependent manner, whic
h has the potential to improve the control of blood sugar levels without the risk of hypoglycemia. | [Definition]
ChEBI: Fasiglifam is a member of biphenyls. | [in vitro]
tak-875 exhibited potent agonist activity and high binding affinity to the human receptor. in addition, tak-875 showed excellent agonist potency selectivity for gpr40 receptor over other members of the ffa receptor family (for which ec50>10 μm) [1]. | [in vivo]
tak-875 showed potent plasma glucose-lowering action and insulinotropic action during an oral glucose tolerance test in female wistar fatty rats with impaired glucose tolerance [2]. | [target]
GPR40 | [References]
[1] negoro n, sasaki s, mikami s, ito m, suzuki m, tsujihata y, ito r, harada a, takeuchi k, suzuki n, miyazaki j, santou t, odani t, kanzaki n, funami m, tanaka t1, kogame a, matsunaga s, yasuma t, momose y. discovery of tak-875: a potent, selective, and orally bioavailable gpr40 agonist. acs med chem lett. 2010 jun 18;1(6):290-4.
[2] leifke e, naik h, wu j, viswanathan p, demanno d, kipnes m, vakilynejad m. a multiple-ascending-dose study to evaluate safety, pharmacokinetics, and pharmacodynamics of a novel gpr40 agonist, tak-875, in subjects with type 2 diabetes. clin pharmacol ther. 2012 jul;92(1):29-39. |
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