BAY 60-6583
Based on 7 publication(s) in Google Scholar
BAY 60-6583 is a potent and high-affinity agonist of adenosine A2B receptor (EC50=3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with Ki values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.67%
- No. CAS: 910487-58-0
- Fòrmula: C19H17N5O2S
- Peso molecular:379.44
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Almacenamiento: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
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) BAY 60-6583
More- Sci Adv. 2022 Dec 23;8(51):eadd3709. [Abstract]
- Br J Pharmacol. 2023 Nov;180(22):2898-2915. [Abstract]
- Biochem Pharmacol. 2025 Sep 20;242(Pt 2):117358. [Abstract]
- J Inflamm Res. 2025 Mar 6:18:3283-3294. [Abstract]
- Placenta. 2025 Dec:172:150-158. [Abstract]
- Tissue Cell. 2022 Aug:77:101828. [Abstract]
- PeerJ. 2023 Aug 30:11:e15922. [Abstract]
Customer Validation & Images
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In Vivo Efficacy Study
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RT-PCR
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Flow Cytometry
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Bio/Physico-chemical Assay
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WB
Ver todos los productos específicos de isoformas Adenosine Receptor
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Actividad biológica
Descripciòn
In Vitro
BAY 60-6583 exhibits EC50 values for receptor activation >10,000 nM for both A1 and A2A AR and 3 nM for A2B AR subtype in CHO cells expressing recombinant human A1, A2A or A2B ARs[1]. BAY 60-6583 (0-10 μM) exhibits the maximum agonist effect of BAY in the absence of siRNA is 68 %, which is significantly different from that in the presence of 5, 50 and 500 nM siRNA (54%, 48% and 36%, respectively). It exhibits EC50 values of BAY in the absence and presence siRNA with 98±22, 102±17, 127±31 and 93±19 nM, respectively, in T24 cells[3]. BAY 60-6583 (5 μM; 24 hours) increases the accumulation of cells at the G1 phase with a decrease in G2/M phase in RAW264.7 preosteoclasts[4]. BAY 60-6583 (5 μM; 24 hours) specifically inhibits the activation of Akt by M-CSF, whereas M-CSF-induced ERK1/2 activation is not affected by BAY 60-6583 treatment in RAW264.7 preosteoclasts[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7 preosteoclasts
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Concentration:5 μM
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Incubation Time:48 hours
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Result:Caused an arrest of cells at the G1 phase.
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Cell Line:RAW264.7 preosteoclasts
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Concentration:5 μM
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Incubation Time:48 hours
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Result:Exhibited an inhibition of M-CSF-mediated Akt activation and resulted in the decrease of osteoclast proliferation.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A2BAR−/− mice on a C57BL/6J mice[1]
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Dosage:2 mg/kg
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Administration:Intraperitoneal injection; 2 mg/kg
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Result:Demonstrated attenuation of lung inflammation and pulmonary edema in wild-type but not in gene-targeted mice for the A2BAR.
Chemical Information
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No. CAS 910487-58-0
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Appearance Solid
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Peso molecular 379.44
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Fòrmula C19H17N5O2S
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Color White to light yellow
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SMILES
O=C(N)CSC1=NC(N)=C(C#N)C(C2=CC=C(OCC3CC3)C=C2)=C1C#N
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Sci Adv
2022 Dec 23;8(51):eadd3709. PMID: 36563137
BAY 60-6583 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2022 Dec 23;8(51):eadd3709. [Abstract]
The potency of BAY60-6583 on the pocket mutations of A2AR.
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Br J Pharmacol
Single cell G-protein coupled receptor profiling of Transcription factor 21 expressing activated kidney fibroblasts. [Abstract]2023 Nov;180(22):2898-2915. PMID: 37115600 -
Biochem Pharmacol
HIF-1α/A2BAR signalling pathway alleviates kidney fibrosis after ischemia-reperfusion injury by preventing macrophage-to-myofibroblast transition. [Abstract]2025 Sep 20;242(Pt 2):117358. PMID: 40983151 -
J Inflamm Res
Adenosine A2A Receptor Activation Alleviated Disease of Mice with Systemic Candida albicans Infection by Regulating Macrophage Function. [Abstract]2025 Mar 6:18:3283-3294. PMID: 40065909
BAY 60-6583 purchased from MedChemExpress. Usage Cited in: J Inflamm Res. 2025 Mar 6:18:3283-3294. [Abstract]
The procedure of mice experiments. Intervention group: CA mice were interpertional with A1R agonist (CCPA), A2AR agonist (GCS21680) or antagonist (KW6002), A2BR agonist (BAY 60–6583) and A3R agonist (2-CI-IB-MECA).
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Placenta
Adenosine promotes trophoblast proliferation without inducing differentiation or apoptosis. [Abstract]2025 Dec:172:150-158. PMID: 41240505 -
Tissue Cell
A1 and A2b adenosine receptors regulate GPX4 against ferroptosis of cardiomyocytes in myocardial infarction rat model and in vitro. [Abstract]2022 Aug:77:101828. PMID: 35653908 -
PeerJ
Co-inhibition of adenosine 2b receptor and programmed death-ligand 1 promotes the recruitment and cytotoxicity of natural killer cells in oral squamous cell carcinoma. [Abstract]2023 Aug 30:11:e15922. PMID: 37663280
BAY 60-6583 purchased from MedChemExpress. Usage Cited in: PeerJ. 2023 Aug 30:11:e15922. [Abstract]
CAL27 cells were treated with BAY60-6583 (A2BR agonist) for 24 h. Real-time quantitative reverse transcription PCR assay showing the mRNA levels of PD-L1 in CAL27 cells after BAY 60-6583 treatment.
BAY 60-6583 purchased from MedChemExpress. Usage Cited in: PeerJ. 2023 Aug 30:11:e15922. [Abstract]
CAL27 cells were treated with BAY60-6583 (A2BR agonist) for 24 h. Flow cytometry assay showing the surface localization of PD-L1 in CAL27 cells after BAY60-6583 treatment.
BAY 60-6583 purchased from MedChemExpress. Usage Cited in: PeerJ. 2023 Aug 30:11:e15922. [Abstract]
CAL27 cells were treated with BAY60-6583 (A2BR agonist) for 24 h. The mean fluorescence intensity of PD-L1 in CAL27 cells after BAY60-6583 treatment.
BAY 60-6583 purchased from MedChemExpress. Usage Cited in: PeerJ. 2023 Aug 30:11:e15922. [Abstract]
CAL27 cells were treated with BAY60-6583 (A2BR agonist) for 24 h. Western blot assay showing the levels of pNF-κ Bp65 after BAY60-6583 treatment.
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (263.55 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)
In Vivo:
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: ≥ 4.17 mg/mL (10.99 mM); Clear solution
This protocol yields a clear solution of ≥ 4.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (41.7 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.
In Vivo Dissolution Calculator
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.
Pureza y Documentación
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Ficha de datos (278 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Aherne CM, et al. Epithelial-specific A2B adenosine receptor signaling protects the colonic epithelial barrier during acute colitis.Mucosal Immunol. 2015 Nov;8(6):1324-38. [Content Brief]
[2]. Schingnitz U, et al. Signaling through the A2B adenosine receptor dampens endotoxin-induced acute lung injury.J Immunol. 2010 May 1;184(9):5271-9. [Content Brief]
[3]. Gao ZG, et al. Probing biased/partial agonism at the G protein-coupled A(2B) adenosine receptor.Biochem Pharmacol. 2014 Aug 1;90(3):297-306. [Content Brief]
[5]. John A. Auchampach, et al. Characterization of the A2B Adenosine Receptor from Mouse, Rabbit, and Dog. J Pharmacol Exp Ther. 2009 Apr;329(1):2-13. [Content Brief]
[6]. Morello S1, et al. Targeting the adenosine A2b receptor in the tumor microenvironment overcomes local immunosuppression by myeloid-derived suppressor cells.Oncoimmunology. 2014 Feb 14;3:e27989. eCollection 2014. [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 | 2.6355 mL | 13.1773 mL | 26.3546 mL | 65.8866 mL |
| 5 mM | 0.5271 mL | 2.6355 mL | 5.2709 mL | 13.1773 mL | |
| 10 mM | 0.2635 mL | 1.3177 mL | 2.6355 mL | 6.5887 mL | |
| 15 mM | 0.1757 mL | 0.8785 mL | 1.7570 mL | 4.3924 mL | |
| 20 mM | 0.1318 mL | 0.6589 mL | 1.3177 mL | 3.2943 mL | |
| 25 mM | 0.1054 mL | 0.5271 mL | 1.0542 mL | 2.6355 mL | |
| 30 mM | 0.0878 mL | 0.4392 mL | 0.8785 mL | 2.1962 mL | |
| 40 mM | 0.0659 mL | 0.3294 mL | 0.6589 mL | 1.6472 mL | |
| 50 mM | 0.0527 mL | 0.2635 mL | 0.5271 mL | 1.3177 mL | |
| 60 mM | 0.0439 mL | 0.2196 mL | 0.4392 mL | 1.0981 mL | |
| 80 mM | 0.0329 mL | 0.1647 mL | 0.3294 mL | 0.8236 mL | |
| 100 mM | 0.0264 mL | 0.1318 mL | 0.2635 mL | 0.6589 mL |
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