MRS-1706
Based on 1 publication(s) in Google Scholar
MRS-1706 is a potent and selective adenosine A2B receptor inverse agonist. MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1 and A3 receptors respectively. MRS-1706 blocks adenosine-mediated cAMP induction.
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- 純度: 98.07%
- CAS 番号: 264622-53-9
- 分子式: C27H29N5O5
- 分子量:503.55
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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 MRS-1706
MoreAdenosine Receptor アイソフォーム固有の製品をすべて表示
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生物活性
Ki: 1.39 (human A2B receptor), 112 (human A2A receptor), 157 (human A1 receptor), 230 nM (human A3 receptor)[2]
MRS-1706 (0.1-5 μM) has antagonist effect of NECA on the wild-type adenosine A2B receptor in a dose-dependent manner[1].
MRS-1706 (0.1-10000 nM) induces inhibition of yeast growth, which yeast cells expressing seven CAM adenosine A2B receptors, with IC50 values of 43, 54, 40, 98, 166, 133 nM for F84L, F84S, F84L/S95G, T42A, T42A/V54A, N36S/T42A, respectively[1].
MRS-1706 (1 μM) inhibits the adenosine-mediated induction of cAMP in wild-type corpus cavernosal strips (CCSs) and decreases the level of cAMP[2].
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.
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Animal Model:Ada–/– mice[2]
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Dosage:1 and 10 μM
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Administration:Intracavernous injection
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Result:Inhibited A2BR signaling and reduced the magnitude and duration.
Inhibited the level of cAMP.
化学情報
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CAS 番号 264622-53-9
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性状 Solid
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分子量 503.55
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分子式 C27H29N5O5
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Color Off-white to yellow
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SMILES
O=C(NC1=CC=C(C(C)=O)C=C1)COC2=CC=C(C3=NC(N(CCC)C(N(CCC)C4=O)=O)=C4N3)C=C2
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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 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
溶剤 & 溶解度
DMSO : 240 mg/mL (476.62 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 6 mg/mL (11.92 mM); Clear solution
This protocol yields a clear solution of ≥ 6 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 6 mg/mL (11.92 mM); Clear solution
This protocol yields a clear solution of ≥ 6 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (273 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Li Q, et, al. ZM241385, DPCPX, MRS1706 are inverse agonists with different relative intrinsic efficacies on constitutively active mutants of the human adenosine A2B receptor. J Pharmacol Exp Ther. 2007 Feb;320(2):637-45. [Content Brief]
[2]. Mi T, et, al. Excess adenosine in murine penile erectile tissues contributes to priapism via A2B adenosine receptor signaling. J Clin Invest. 2008 Apr;118(4):1491-501. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9859 mL | 9.9295 mL | 19.8590 mL | 49.6475 mL |
| 5 mM | 0.3972 mL | 1.9859 mL | 3.9718 mL | 9.9295 mL | |
| 10 mM | 0.1986 mL | 0.9930 mL | 1.9859 mL | 4.9648 mL | |
| 15 mM | 0.1324 mL | 0.6620 mL | 1.3239 mL | 3.3098 mL | |
| 20 mM | 0.0993 mL | 0.4965 mL | 0.9930 mL | 2.4824 mL | |
| 25 mM | 0.0794 mL | 0.3972 mL | 0.7944 mL | 1.9859 mL | |
| 30 mM | 0.0662 mL | 0.3310 mL | 0.6620 mL | 1.6549 mL | |
| 40 mM | 0.0496 mL | 0.2482 mL | 0.4965 mL | 1.2412 mL | |
| 50 mM | 0.0397 mL | 0.1986 mL | 0.3972 mL | 0.9930 mL | |
| 60 mM | 0.0331 mL | 0.1655 mL | 0.3310 mL | 0.8275 mL | |
| 80 mM | 0.0248 mL | 0.1241 mL | 0.2482 mL | 0.6206 mL | |
| 100 mM | 0.0199 mL | 0.0993 mL | 0.1986 mL | 0.4965 mL |
MRS-1706 関連分類
HY-103186 関連分類
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