GS-6201
Based on 1 publication(s) in Google Scholar
GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM). GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice.
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- 純度: 98.47%
- CAS 番号: 752222-83-6
- 分子式: C21H21F3N6O2
- 分子量:446.43
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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 GS-6201
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: 22 nM (human A2B receptors), 1070 nM (human A3 receptors), 1940 nM (human A1 receptors), 3280 nM (human A2A receptors)[1]
GS-6201 (4 mg/kg; i.p.; every 12 h for 14 days) leads to a significant attenuation of left and right ventricular enlargement and dysfunction at 7 days, which was maintained at 14 days and also at 28 days[2].
GS-6201 (2 mg/kg; p.o.) treatment shows the Cmax, dAUC and t1/2 are 1110 ng/mL, 6500 ng h/mL, and 4.25 hours, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult out-bred male CD1 mice (8-12 weeks of age, AMI model)[2]
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Dosage:4 mg/kg
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Administration:i.p.; every 12 h for 14 days
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Result:Significantly reduced IL-6, TNF-α, E-selectin, ICAM-1, and VCAM plasma levels.
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Animal Model:Sprague-Dawley rats[1]
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Dosage:2 mg/kg
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Administration:p.o. (Pharmacokinetic Analysis)
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Result:The Cmax, dAUC and t1/2 were 1110 ng/mL, 6500 ng h/mL, and 4.25 hours, respectively.
化学情報
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CAS 番号 752222-83-6
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性状 Solid
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分子量 446.43
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分子式 C21H21F3N6O2
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Color White to light brown
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SMILES
O=C(N1CCC)N(CC)C2=C(N=C(C3=CN(CC4=CC=CC(C(F)(F)F)=C4)N=C3)N2)C1=O
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別名
CVT-6883
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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 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
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Nat Commun
Transcriptional control of pancreatic cancer immunosuppression by metabolic enzyme CD73 in a tumor-autonomous and -autocrine manner. [Abstract]2023 Jun 8;14(1):3364. PMID: 37291128
溶剤 & 溶解度
DMSO : 100 mg/mL (224.00 mM; ultrasonic and warming and heat to 60°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, 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: 2 mg/mL (4.48 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 (274 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Elzein E, et al. Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases. J Med Chem. 2008 Apr 10;51(7):2267-78. [Content Brief]
[2]. Toldo S, et al. GS-6201, a selective blocker of the A2B adenosine receptor, attenuates cardiac remodeling after acute myocardial infarction in the mouse. J Pharmacol Exp Ther. 2012 Dec;343(3):587-95. [Content Brief]
[3]. Mustafa SJ, et al. Effect of a specific and selective A(2B) adenosine receptor antagonist on adenosine agonist AMP and allergen-induced airway responsiveness and cellular influx in a mouse model of asthma. J Pharmacol Exp Ther. 2007 Mar;320(3):1246-51. [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 | 2.2400 mL | 11.2000 mL | 22.3999 mL | 55.9998 mL |
| 5 mM | 0.4480 mL | 2.2400 mL | 4.4800 mL | 11.2000 mL | |
| 10 mM | 0.2240 mL | 1.1200 mL | 2.2400 mL | 5.6000 mL | |
| 15 mM | 0.1493 mL | 0.7467 mL | 1.4933 mL | 3.7333 mL | |
| 20 mM | 0.1120 mL | 0.5600 mL | 1.1200 mL | 2.8000 mL | |
| 25 mM | 0.0896 mL | 0.4480 mL | 0.8960 mL | 2.2400 mL | |
| 30 mM | 0.0747 mL | 0.3733 mL | 0.7467 mL | 1.8667 mL | |
| 40 mM | 0.0560 mL | 0.2800 mL | 0.5600 mL | 1.4000 mL | |
| 50 mM | 0.0448 mL | 0.2240 mL | 0.4480 mL | 1.1200 mL | |
| 60 mM | 0.0373 mL | 0.1867 mL | 0.3733 mL | 0.9333 mL | |
| 80 mM | 0.0280 mL | 0.1400 mL | 0.2800 mL | 0.7000 mL | |
| 100 mM | 0.0224 mL | 0.1120 mL | 0.2240 mL | 0.5600 mL |
GS-6201 関連分類
HY-10081 関連分類
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