Adenosine A1 receptor activator T62
Based on 1 publication(s) in Google Scholar
Adenosine A1 receptor activator T62 is an allosteric enhancer of adenosine A1 receptor. Adenosine A1 receptor activator T62 produces antinociception in animal models of acute pain and also reduces hypersensitivity in models of inflammatory and nerve-injury pain.
For research use only. We do not sell to patients.
- Purity: 98.93%
- CAS No.: 40312-34-3
- Formula: C15H14ClNOS
- Molecular Weight:291.80
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Adenosine A1 receptor activator T62
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Biological Activity
Description
IC50 & Target
Adenosine A1 receptor[1]
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male SpragueDawley rats (250 g) after paw incision surgery[1]
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Dosage:0.3 μg, 0.5 μg, 1 μg, and 3 μg
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Administration:Intrathecal administration
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Result:Produced a dose-dependent antihypersensitivity effect, with no effect on ambulation or activity level. The ED40 (95% confidence interval) was 0.77 (0.63-0.91) μg.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 40312-34-3
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Appearance Solid
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Molecular Weight 291.80
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Formula C15H14ClNOS
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Color Light yellow to yellow
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SMILES
O=C(C1=CC=C(Cl)C=C1)C2=C(N)SC3=C2CCCC3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (342.70 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.
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: ≥ 2.5 mg/mL (8.57 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.
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.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Obata H, et al. Spinal adenosine receptor activation reduces hypersensitivity after surgery by a different mechanism than after nerve injury. Anesthesiology. 2004 May;100(5):1258-62. [Content Brief]
[2]. Li X, et al. Allosteric adenosine receptor modulation reduces hypersensitivity following peripheral inflammation by a central mechanism. J Pharmacol Exp Ther. 2003 Jun;305(3):950-5. [Content Brief]
[3]. Soudijn W, et al. Allosteric modulation of G protein-coupled receptors: perspectives and recent developments. Drug Discov Today. 2004 Sep 1;9(17):752-8. [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 | 3.4270 mL | 17.1350 mL | 34.2700 mL | 85.6751 mL |
| 5 mM | 0.6854 mL | 3.4270 mL | 6.8540 mL | 17.1350 mL | |
| 10 mM | 0.3427 mL | 1.7135 mL | 3.4270 mL | 8.5675 mL | |
| 15 mM | 0.2285 mL | 1.1423 mL | 2.2847 mL | 5.7117 mL | |
| 20 mM | 0.1714 mL | 0.8568 mL | 1.7135 mL | 4.2838 mL | |
| 25 mM | 0.1371 mL | 0.6854 mL | 1.3708 mL | 3.4270 mL | |
| 30 mM | 0.1142 mL | 0.5712 mL | 1.1423 mL | 2.8558 mL | |
| 40 mM | 0.0857 mL | 0.4284 mL | 0.8568 mL | 2.1419 mL | |
| 50 mM | 0.0685 mL | 0.3427 mL | 0.6854 mL | 1.7135 mL | |
| 60 mM | 0.0571 mL | 0.2856 mL | 0.5712 mL | 1.4279 mL | |
| 80 mM | 0.0428 mL | 0.2142 mL | 0.4284 mL | 1.0709 mL | |
| 100 mM | 0.0343 mL | 0.1714 mL | 0.3427 mL | 0.8568 mL |