AR 231453
Based on 3 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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.58%
- CAS 番号: 733750-99-7
- 分子式: C21H24FN7O5S
- 分子量:505.52
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
HY-15291
MBX-2982GPR119 Agonist -
HY-12764
6-OAUGPR84 Agonist -
HY-N2327
OleamideEndogenous Metabolite -
HY-107535
AS1269574GPR119 Agonist -
HY-15589
GW9508GPR40 Agonist -
HY-15565
APD668GPR119 Agonist -
HY-12066
GSK1292263 -
HY-15566
APD597GPR119 Agonist -
HY-16673
PSN632408GPR119 Agonist -
HY-15564R
AR 231453 (Standard)GPR119 Agonist -
HY-W011121
2-OleoylglycerolGPR119 Agonist -
HY-15291R
MBX-2982 (Standard)GPR119 Agonist
MedChemExpress（MCE）の使用を引用している文献 AR 231453
More
生物活性
製品説明
Cellular Effect
|
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] |
体外実験
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.
体内実験
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.
化学情報
-
CAS 番号 733750-99-7
-
性状 Solid
-
分子量 505.52
-
分子式 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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
-
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 Nov:241:117095. PMID: 40617490 -
Structure
2026 Jun 10:S0969-2126(26)00153-X. PMID: 42269610
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
取扱説明書 (2659 KB)
参考文献
[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 |
AR 231453 関連分類
HY-15564 関連分類
Powered by Bioz