[CAS NO. 733750-99-7] AR231453
PRODUCTS SPECIFICATIONS [733750-99-7]
DESCRIPTION [733750-99-7]
Overview
| MDL | MFCD14706714 |
|---|---|
| Molecular Weight | 505.52 |
| Molecular Formula | C21H24FN7O5S |
| SMILES | CC(C)C1=NOC(C2CCN(C3=NC=NC(NC4=CC=C(S(=O)(C)=O)C=C4F)=C3[N+]([O-])=O)CC2)=N1 |
1 Publications Citing Use of MCE
Summary
In Vitro
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 (EC
50
= 4.7 nM) with a maximal efficacy similar to that seen with forskolin. AR 231453 significantly enhancesinsulin release in HIT-T15 cells, with an EC
50
of 3.5 nM
[1]
.
AR 231453 also stimulates insulin release in isolated mouse islets at glucose concentrations ranging from 8-17 mM
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Mice [1] . |
| Dosage: | 20 mg/kg. |
| Administration: | Orally, once. |
| Result: | Improved glucose tolerance in mice. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 25 mg/mL ( 49.45 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9782 mL | 9.8908 mL | 19.7816 mL |
| 5 mM | 0.3956 mL | 1.9782 mL | 3.9563 mL |
| 10 mM | 0.1978 mL | 0.9891 mL | 1.9782 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (4.95 mM); Suspended solution; Need ultrasonic
References
- [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.
Synonyms