CAS NO: | 306974-70-9 |
规格: | 98% |
分子量: | 520.59 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
Background:
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, respectively1.
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 secretion1. 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 GPR1202.
参考文献:
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