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Signal Inhibitors and Activators
TAK-875
$816/ 5mg
QuantityTotal: $816
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Product Information
Kinase Inhibitor Name TAK-875
FormulaC29H32O7S.1/2H2O
SolubilityDMSO ≥105 mg/mL Water <1 mg/mL Ethanol ≥11 mg/mL
Stability:
2 years -20℃ Powder
1 week -4℃ in DMSO
1 month -80℃ in DMSO
Stability:
2 years -20℃ Powder
1 week -4℃ in DMSO
1 month -80℃ in DMSO
CAS No.1000413-72-8
Biological ActivityTAK-875 is a potent, selective and orally bioavailable GPR40 agonist with an EC50 of 0.072 μM. TAK-875 is a new agent applied in the treatment of type 2 diabetes. TAK-875 not only elevated the levels of intra-cellular inositol monophosphate as well as calcium contents in rat insulinoma INS-1 833/15 cells but also improved the tolerance of glucose and amplified insulin secretion when orally administered in tolerance test. However, TAK-875 didn’t increase the secretion of insulin and cause hypoglycemia when 30 mg/kg dosage of TAK-875 was given in fasted normal Sprague Dawley rats. Conversely, TAK-875 with a dosage of 10 mg/kg (p.o.) not only significantly improved plasma insulin levels but also decreased fasting hyperglycemia in male Zucker diabetic fatty rats. [1][2]
M.W.533.63
ReferencesTAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats. Tsujihata Y et al. J Pharmacol Exp Ther. 2011 Jul 13
The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.
The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.
Price816$
Research AreaStem Cells Cancer Cardiovascular Cell Biology Epigenetics & Nuclear Signaling Developmental Biologys Immunology Drug Discovery Products Metabolism Neuroscience Signal Transduction
is a potent, selective and orally bioavailable GPR40 agonist with an EC50 of a new agent applied in the treatment of type 2 diabetes. TAK-875 not only elevated the inositol monophosphate as well as calcium contents in rat insulinoma INS-1 833/15 improved the tolerance of glucose and amplified insulin secretion when orally administered However, TAK-875 didn’t increase the secretion of insulin and cause hypoglycemia dosage of TAK-875 was given in fasted normal Sprague Dawley rats. Conversely, TAK-875
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