| Bioactivity | AR 231453 is a potent, specific and orally available GPR119 agonist. AR 231453 can stimulate β-cell replication and improve islet graft function s[1][2]. | ||||||||||||
| Invitro | AR 231453 is inactive at all other GPCRs tested (more than 230, including all known pancreatic islet receptors), indicating that it is highly selective for GPR119[1].AR 231453 potently stimulats cAMP accumulation (EC50 = 4.7 nM) with a maximal efficacy similar to that seen with forskolin. AR 231453 significantly enhancesinsulin release in HIT-T15 cells, with an EC50 of 3.5 nM[1].AR 231453 also stimulates insulin release in isolated mouse islets at glucose concentrations ranging from 8-17 mM[1]. | ||||||||||||
| In Vivo | AR231453 (20 mg/kg, orally) markedly improves oral glucose tolerance in a dose-dependent fashion, with efficacy similar to maximally effective doses of the sulfonylurea glyburide[1]. Animal Model: | ||||||||||||
| Name | AR 231453 | ||||||||||||
| CAS | 733750-99-7 | ||||||||||||
| Formula | C21H24FN7O5S | ||||||||||||
| Molar Mass | 505.52 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Chu ZL, et al. A role for beta-cell-expressed G protein-coupled receptor 119 in glycemic control by enhancing glucose-dependent insulin release. Endocrinology. 2007 Jun;148(6):2601-9. [2]. J Gao, et al. Stimulating β-cell replication and improving islet graft function by AR231453, A GPR119 agonist. Transplant Proc. 2011 Nov;43(9):3217-20. |
AR 231453
CAS: 733750-99-7 F: C21H24FN7O5S W: 505.52
AR 231453 is a potent, specific and orally available GPR119 agonist. AR 231453 can stimulate β-cell replication and imp
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.