(rel)-AR234960
Based on 1 publication(s) in Google Scholar
(rel)-AR234960 is a selective and competitive agonist of the G protein-coupled receptor MAS. (rel)-AR234960 binds to the MAS receptor to activate the downstream ERK1/2 signaling pathway, inducing the expression of connective tissue growth factor (CTGF) and its downstream collagen subtype genes (such as COL1A1, COL3A1). (rel)-AR234960 promotes collagen synthesis in cardiac fibroblasts through the MAS-ERK1/2-CTGF pathway and aggravates extracellular matrix remodeling. (rel)-AR234960's in vitro effect can be blocked by the MAS inverse agonist AR244555 and MEK1 inhibitor. (rel)-AR234960 regulates the expression of cardiac fibrosis-related genes and can be used in the study of heart failure.
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- 純度: 98.95%
- CAS 番号: 1408311-94-3
- 分子式: C27H30FN5O5S
- 分子量:555.62
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 (rel)-AR234960
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生物活性
AR234960 (10 μM; 12 h) activates the MAS receptor in HEK293-MAS cells, induces the expression of CTGF and collagen genes COL1A1 and COL4A1, and activates ERK1/2 phosphorylation[2].
AR234960 (10 μM; 12 h) induces the expression of CTGF, COL1A2, and COL3A1 in adult human cardiac fibroblasts (HCF), which effect can be completely blocked by the MAS inverse agonist AR244555 (HY-111273) or the MEK1 inhibitor PD98059 (HY-12028)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1408311-94-3
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性状 Solid
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分子量 555.62
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分子式 C27H30FN5O5S
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Color White to off-white
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SMILES
O=S(N1C[C@@H](CN2CCN(C3=NC=CC=C3)CC2)[C@H](C4=CC=CC(F)=C4)C1)(C5=CC=C([N+]([O-])=O)C=C5OC)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Mol Life Sci
Suppression of Skp2 contributes to sepsis-induced acute lung injury by enhancing ferroptosis through the ubiquitination of SLC3A2. [Abstract]2024 Jul 30;81(1):325. PMID: 39079969
溶剤 & 溶解度
DMSO : 25 mg/mL (44.99 mM; ultrasonic and heat to 80°C; 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.50 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (278 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Chen Z, et al. Suppression of Skp2 contributes to sepsis-induced acute lung injury by enhancing ferroptosis through the ubiquitination of SLC3A2. Cell Mol Life Sci. 2024 Jul 30;81(1):325. [Content Brief]
[2]. Chatterjee A, et al. Connective tissue growth factor dependent collagen gene expression induced by MAS agonist AR234960 in human cardiac fibroblasts. PLoS One. 2017 Dec 29;12(12):e0190217. [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 | 1.7998 mL | 8.9990 mL | 17.9979 mL | 44.9948 mL |
| 5 mM | 0.3600 mL | 1.7998 mL | 3.5996 mL | 8.9990 mL | |
| 10 mM | 0.1800 mL | 0.8999 mL | 1.7998 mL | 4.4995 mL | |
| 15 mM | 0.1200 mL | 0.5999 mL | 1.1999 mL | 2.9997 mL | |
| 20 mM | 0.0900 mL | 0.4499 mL | 0.8999 mL | 2.2497 mL | |
| 25 mM | 0.0720 mL | 0.3600 mL | 0.7199 mL | 1.7998 mL | |
| 30 mM | 0.0600 mL | 0.3000 mL | 0.5999 mL | 1.4998 mL | |
| 40 mM | 0.0450 mL | 0.2250 mL | 0.4499 mL | 1.1249 mL |
(rel)-AR234960 関連分類
HY-120006A 関連分類
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