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TAK-875 (CAS 1000413-72-8) LS-H136

FFAR1 agonist
LS-H136-500 / 500 µg / $185
LS-H136-1000 / 1000 µg / $205
LS-H136-5000 / 5000 µg / $335
LS-H136-10000 / 10000 µg / $405
USA Shipment Only
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Description: The free fatty acid receptor 1 (FFAR1; GPR40) is highly expressed in pancreatic beta -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). H136_ChemicalStructureImage.png
(3S)-6-[[2',6'-dimethyl-4'-[3-(methylsulfonyl)propoxy][1,1'-biphenyl]-3-yl]methoxy]-2,3-dihydro-3-benzofuranacetic acid
 
biochemical, chemical, agonist
LS-H136
1000413-72-8
C29H32O7S
≥95%
A crystalline solid
 
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
InChI=1S/C29H32O7S/c1-19-12-25(34-10-5-11-37(3,32)33)13-20(2)29(19)22-7-4-6-21(14-22)17-35-24-8-9-26-23(15-28(30)31)18-36-27(26)16-24/h4,6-9,12-14,16,23H,5,10-11,15,17-18H2,1-3H3,(H,30,31)/t23-/m1/s1
BZCALJIHZVNMGJ-HSZRJFAPSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: FFAR1 / GPR40 related products

Usage Information

TAK-875 is supplied as a crystalline solid. A stock solution may be made by dissolving the TAK-875 in the solvent of choice. TAK-875 is soluble in organic solvents such as DMSO and dimethyl formamide, which should be purged with an inert gas. The solubility of TAK-875 in these solvents is approximately 30 mg/ml. TAK-875 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, TAK-875 should first be dissolved in DMSO and then diluted with the aqueous buffer of choice. TAK-875 has a solubility of approximately 0.5 mg/ml in a 1:1 solution of DMSO:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Briscoe, C.P., Tadayyon, M., Andrews, J.L., et al. The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids. J. Biol. Chem. 278(13), 11303-11311 (2003).
  2. Itoh, Y., Kawamata, Y., Harada, M., et al. Free fatty acids regulate insulin secretion from pancreatic β cells through GPR40. Nature 422, 173-176 (2003).
  3. Steneberg, P., Rubins, N., Bartoov-Shifman, R., et al. The FFA receptor GPR40 links hyperinsulinemia, hepatic steatosis, and impaired glucose homeostasis in mouse. Cell Metab. 1, 245-258 (2005).
  4. Christiansen, E., Due-Hansen, M.E., Urban, C., et al. Free fatty acid receptor 1 (FFA1/GPR40) agonists: Mesylpropoxy appendage lowers lipophilicity and improves ADME properties. J. Med. Chem. 55, 6624-6628 (2012).

 


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