AR 231453
Based on 2 publication(s) in Google Scholar
AR 231453 is a potent, specific and orally available GPR119 agonist. AR 231453 can stimulate β-cell replication and improve islet graft function s.
For research use only. We do not sell to patients.
- Purity: 99.58%
- CAS No.: 733750-99-7
- Formula: C21H24FN7O5S
- Molecular Weight:505.52
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
GPCR/G Protein Compound Library
HY-L006
-
Neuronal Signaling Compound Library
HY-L013
-
Orally Active Compound Library
HY-L061
-
Human Metabolite Library
HY-L123
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Highly Selective Activators Library
HY-L159
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Lactylation Compound Library
HY-L249
Publications Citing Use of MedChemExpress (MCE) AR 231453
More
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.003 mM
Compound: 1, AR231453
|
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
|
[PMID: 24751443] |
| HEK293 | EC50 |
0.7 μM
Compound: 2; AR231453
|
Agonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assay
Agonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assay
|
[PMID: 27560285] |
| HEK293 | EC50 |
4.78 nM
Compound: AR231543
|
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
|
[PMID: 31630858] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (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.
Chemical Information
-
CAS No. 733750-99-7
-
Appearance Solid
-
Molecular Weight 505.52
-
Formula C21H24FN7O5S
-
Color Light yellow to yellow
-
SMILES
CC(C)C1=NOC(C2CCN(C3=NC=NC(NC4=CC=C(S(=O)(C)=O)C=C4F)=C3[N+]([O-])=O)CC2)=N1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
Nat Commun
2022 Nov 17;13(1):7033. PMID: 36396650 -
Biochem Pharmacol
The C-terminal region regulates the constitutive signaling activity of GPR119: G protein recruitment. [Abstract]2025 Jul 3:241:117095. PMID: 40617490
Solvent & Solubility
DMSO : 25 mg/mL (49.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (273 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9782 mL | 9.8908 mL | 19.7816 mL | 49.4540 mL |
| 5 mM | 0.3956 mL | 1.9782 mL | 3.9563 mL | 9.8908 mL | |
| 10 mM | 0.1978 mL | 0.9891 mL | 1.9782 mL | 4.9454 mL | |
| 15 mM | 0.1319 mL | 0.6594 mL | 1.3188 mL | 3.2969 mL | |
| 20 mM | 0.0989 mL | 0.4945 mL | 0.9891 mL | 2.4727 mL | |
| 25 mM | 0.0791 mL | 0.3956 mL | 0.7913 mL | 1.9782 mL | |
| 30 mM | 0.0659 mL | 0.3297 mL | 0.6594 mL | 1.6485 mL | |
| 40 mM | 0.0495 mL | 0.2473 mL | 0.4945 mL | 1.2364 mL |
Powered by Bioz