TAK875 Chemical Properties

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)

pka

4.36±0.10(Predicted)

form 

Solid

color 

White to Off-White

TAK875 Usage And Synthesis

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. 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. 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).

Uses

TAK-876 is a selective G protein-coupled receptor 40 (GPR40) agonist (1,2). TAK-876 is a novel oral medication that has been developed to improve the secretion of insulin in a glucose-dependent manner, which has the potential to improve the control of blood sugar levels with a low risk of hypoglycemia.

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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