GW-1100 (Synonyms: GW1100;GW1100) |
Katalog-Nr.GC14027 |
A selective GPR40 antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 306974-70-9
Sample solution is provided at 25 µL, 10mM.
GW1100 is a selective GPR40 antagonist. It dose dependently inhibited GPR40-mediated Ca2+ elevations stimulated by GW9508 and linoleic acid with pIC50 values of 5.9970.03 and 5.9970.06, respectively 1.
GW1100 inhibited the Ca2+ elevations stimulated by GW9508 mediated by GPR40, but not those mediated via GPR120 by either GW9508 or linoleic acid, demonstrating that GW1100 was a selective antagonist of the GPR40 receptor. GW1100 reversed the effects of GW9508 on insulin secretion, but only partially attenuated linoleic acid-stimulated insulin secretion 1. Ishikawa cells were treated with a GPR40 antagonist, GW1100, in conjunction with GW9508. GW1100 had no effect on the stimulation of cell proliferation, suggesting all pro-proliferative effects of GW9508 are mediated through GPR120 2.
References:
1. Briscoe CP, Peat AJ, McKeown SC et al. Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol. 2006 Jul;148(5):619-28.
2. http://www.aups.org.au/Proceedings/41/44P
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