TAK-875 hymihydrate
TAK-875
CAS: 1374598-80-7
Molecular Formula: C58H66O15S2
TAK-875 hymihydrate - Names and Identifiers
| Name | TAK-875 |
| Synonyms | TAK875 TAK-875 CS-1926 TAK-875(0.5H2O) TAK875 hemihydrate TAK-875 hymihydrate [(3S)-6-({2',6'-dimethyl-4'-[3-(methylsulfonyl)propoxy]biphe-nyl-3-yl}meth-oxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid hemi-hydrate TAK875 (3S)-6-[[2',6'-Dimethyl-4'-[3-(methylsulfonyl)propoxy][1,1'-biphenyl]-3-yl]methoxy]-2,3-dihydro-3-benzofuranacetic acid |
| CAS | 1374598-80-7 |
TAK-875 hymihydrate - Physico-chemical Properties
| Molecular Formula | C58H66O15S2 |
| Molar Mass | 1067.26564 |
| Storage Condition | -20℃ |
| In vitro study | TAK-875 exhibits potent agonist activity and high binding affinity to the human GPR40 receptor with Ki of 38 nM. TAK-875 displays weaker affinity toward the rat GPR40 receptor with Ki of 140 nM. TAK-875 displays excellent selectivity as TAK-875 has little agonist potency to other members of the FFA receptor family with EC50 of >10 μM. TAK-875 treatment induces a concentration-dependent increase in intracellular IP production in CHO-hGPR40 with EC50 of 72 nM, more potently than that endogenous ligand agonist oleic acid which requires much higher ligand concentrations to activate the receptor with EC50 of 29.9 μM. Neither TAK-875 nor oleic acid elicits an IP response in control CHO cells devoid of hGPR40. Consistent with the activation of Gqα-mediated signaling pathway, TAK-875. Prolonged suppression of GPR40/FFA1 by TAK-875 does not cause dramatic beta Cell dysfunction or induction of apotosis. TAK-875 showed potent agonist activity and high binding affinity to human GPR40 receptor with K I of 38 nM. TAK-875 showed a weak affinity for the rat GPR40 receptor with a K I of 140 nM. TAK-875 showed good selectivity with little agonistic effect on other members of the FFA receptor family with an EC50 >10 μm. TAK-875 treatment induced a concentration-dependent increase in intracellular IP production in CHO-hGPR40 with an EC50 of 72 nM, the Agonist oleic acid (EC50 of 29.9 μm) was more potent than the one that required higher ligand concentrations to activate the endogenous ligand of the receptor. Neither TAK-875 nor oleic acid could induce an IP response in hGPR40-deficient control CHO cells. Consistent with gqα-mediated signaling pathway activation, TAK-875 increased glucose-dependent insulin secretion in pancreatic beta cells. TAK-875 prolonged stimulation of GPR40/FFA1 did not cause islet β-cell dysfunction or induce apoptosis. |
| In vivo study | In a rat model of diabetes, single oral dosing of TAK-875 at 0.3-3 mg/kg reduces the blood glucose excursion and augments insulin secretion during an oral glucose tolerance test, when TAK-875 is administered 1 hour before an oral glucose challenge. In type 2 diabetic N-STZ-1.5 rats, administration of TAK-875 (1-10 mg/kg p.o.) Show a clear improvement in glucose tolerance and inclusions. Additive, ask -875 (10 mg/kg, p.o.) significance augmentations plasma insulin levels and reduction connecting hyperglycemia in male Zucker diabetic fatty rats, all in fast normal Sprague-Dawley rats, TAK-875. in a diabetic rat model, a single oral dose of 0.3-3 mg/kg TAK-875 Administration reduced blood glucose excursion, and TAK-875 administration increased insulin secretion in an oral glucose tolerance test one hour prior to oral glucose stimulation. In type 2 diabetic N-STZ-1.5 rats, TAK-875(1-10 mg/kg p.o.) administration significantly improved glucose tolerance and increased insulin secretion. In addition, in male Zucker diabetic obese rats, TAK-875 (10 mg/kg, p.o.) significantly increased plasma insulin levels and reduced fasting hyperglycemia, whereas in fasted normal Sprague-Dawley rats, TAK-875 did not enhance insulin secretion and did not cause hypoglycemia even at the 30 mg/kg dose. |
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Product Name: TAK-875 Visit Supplier Webpage Request for quotation
CAS: 1374598-80-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1374598-80-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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