Regadenoson
Based on 3 publication(s) in Google Scholar
Regadenoson (CVT-3146) is a selective A2A adenosine receptor agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of agents to the human CNS.
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- Purity: 98.83%
- CAS No.: 313348-27-5
- 화학식: C15H18N8O5
- 분자량:390.35
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Regadenoson
MoreAll Adenosine Receptor Isoforms
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Biological Activity
? Regadenoson (2.5 μg/kg; p.i.v.; single in 30 s) increases blood flow of coronary in awake dogs[1].
? Regadenoson (0.5 μg/kg; i.v.; single; 60 or 90 min after Temozolomide administration) promotes Temozolomide delivery to CNS of rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mongrel dogs (23-27 kg)[1]
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Dosage:0.1, 0.175, 0.25, 0.5, 1.0, 2.5, 5 µg/kg
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Administration:Peripheral intravenous injection; single.
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Result:Increased mean CBF (coronary blood flow) in a dose-dependent manner, with an ED50 of 0.34 µg/kg and resulted in a maximal increase of 154 mL/min from baseline (45 mL/min).
Caused a dose-dependent decrease in mean coronary resistance with a maximal decrease of 73 and 75 % at 2.5 and 5 µg/kg, respectively.
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Animal Model:Mongrel dogs (23-27 kg)[1]
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Dosage:2.5 µg/kg
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Administration:Peripheral intravenous injection; single in 30 s.
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Result:Reached 84% of the peak reactive hyperemia flow following a 20-s-long coronary occlusion (201 mL/min).
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Animal Model:Female F344 rats (150-170 g)[2]
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Dosage:0.5 µg/kg
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Administration:Intravenous injection; single (60 or 90 min after Temozolomide administration)
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Result:Increaseed levels of Temozolomide by 60 % in normal brain without affecting plasma concentrations.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 313348-27-5
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Appearance Solid
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분자량 390.35
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화학식 C15H18N8O5
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Color White to off-white
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SMILES
OC[C@@H]1[C@@H](O)[C@@H](O)[C@H](N2C3=C(N=C2)C(N)=NC(N4C=C(C=N4)C(NC)=O)=N3)O1
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Synonyms
CVT-3146
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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J Cell Commun Signal
Lactate drives CD38 signaling to promote Epithelial-Mesenchymal Transition through Snail induction in non-small cell lung cancer cells. [Abstract]2024 Feb 14;18(1):e12018. PMID: 38545257 -
Turk J Med Sci
Contribution of adenosine A2A receptor agonist and antagonist on ovarian ischemia/reperfusion injury in rats. [Abstract]2025 Dec 31;56(1):364-376. PMID: 41816720 -
bioRxiv
Host GPCR-cAMP signaling balances Gαs and Gαi activity to control intracellular Brucella infection. [Abstract]2026 Jan 6:2026.01.06.697936. PMID: 41542404
용액&용해도
DMSO : 50 mg/mL (128.09 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)
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 (6.40 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.40 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 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.
순도&문서
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Data Sheet (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)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Trochu JN, et al. Selective A2A adenosine receptor agonist as a coronary vasodilator in conscious dogs: potential for use in myocardial perfusion imaging. J Cardiovasc Pharmacol. 2003 Jan;41(1):132-9. [Content Brief]
[2]. Jackson S, et al. The effect of regadenoson-induced transient disruption of the blood-brain barrier on temozolomide delivery to normal rat brain. J Neurooncol. 2016 Feb;126(3):433-9. [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 | 2.5618 mL | 12.8090 mL | 25.6180 mL | 64.0451 mL |
| 5 mM | 0.5124 mL | 2.5618 mL | 5.1236 mL | 12.8090 mL | |
| 10 mM | 0.2562 mL | 1.2809 mL | 2.5618 mL | 6.4045 mL | |
| 15 mM | 0.1708 mL | 0.8539 mL | 1.7079 mL | 4.2697 mL | |
| 20 mM | 0.1281 mL | 0.6405 mL | 1.2809 mL | 3.2023 mL | |
| 25 mM | 0.1025 mL | 0.5124 mL | 1.0247 mL | 2.5618 mL | |
| 30 mM | 0.0854 mL | 0.4270 mL | 0.8539 mL | 2.1348 mL | |
| 40 mM | 0.0640 mL | 0.3202 mL | 0.6405 mL | 1.6011 mL | |
| 50 mM | 0.0512 mL | 0.2562 mL | 0.5124 mL | 1.2809 mL | |
| 60 mM | 0.0427 mL | 0.2135 mL | 0.4270 mL | 1.0674 mL | |
| 80 mM | 0.0320 mL | 0.1601 mL | 0.3202 mL | 0.8006 mL | |
| 100 mM | 0.0256 mL | 0.1281 mL | 0.2562 mL | 0.6405 mL |
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