EOS-984
Based on 1 Customer Validation
EOS-984 is a macrocyclic diamine equilibrative nucleoside transporter 1 (ENT1) inhibitor. EOS984 inhibits ENT1 and ENT1-mediated nucleoside transport, restricting adenosine entry into cells via ENT1, thereby attenuating ATP-derived adenosine-mediated T cell immunosuppression and restoring primary human T cell proliferation. EOS984 can be used in research related to ENT1-mediated nucleoside transport, adenosine-related immunosuppression, and tumor immunity.
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- Pureté : 99.98%
- CAS No.: 2724937-55-5
- Formule: C33H47N3O9
- Masse moléculaire:629.74
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Stockage:Powder -20°C, 3 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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
ENT1 |
In Vitro
EOS-984 (compound 10) (up to 100 μM; 90 s) inhibits hERG current in CHO cells stably expressing the hERG ion channel with an IC50 of 3.4 μM[1].
EOS-984 (30 min pre-incubation) inhibits human ENT1 probe binding in JAR cells, with an IC50 activity rating of ++ and an IC50 of 0.001-0.02 μM[1].
EOS-984 inhibits ENT1-mediated uridine transport in MDCKII-ENT1-LV cells stably expressing human ENT1, with an IC50 activity category of ++[1].
EOS-984 restores proliferation of activated primary human CD3+ T cells under high protein binding conditions, with a T Cell Proliferation IC50 activity bin of + in Condition B[1].
EOS-984 restores ATP-mediated inhibition of proliferation in activated primary human CD3+ T cells, with a T Cell Proliferation IC50 activity rating of ++ under Condition A[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2724937-55-5
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Appearance Solid
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Masse moléculaire 629.74
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Formule C33H47N3O9
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Color White to off-white
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SMILES
COC1=CC(C(O[C@@H]2CCCOC3=C(C(OC)=CC(C(NCCCN4CCCN(CC4)CC2)=O)=C3)OC)=O)=CC(OC)=C1OC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 175 mg/mL (277.89 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: ≥ 8.75 mg/mL (13.89 mM); Clear solution
This protocol yields a clear solution of ≥ 8.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (87.5 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.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 1.5880 mL | 7.9398 mL | 15.8796 mL | 39.6989 mL |
| 5 mM | 0.3176 mL | 1.5880 mL | 3.1759 mL | 7.9398 mL | |
| 10 mM | 0.1588 mL | 0.7940 mL | 1.5880 mL | 3.9699 mL | |
| 15 mM | 0.1059 mL | 0.5293 mL | 1.0586 mL | 2.6466 mL | |
| 20 mM | 0.0794 mL | 0.3970 mL | 0.7940 mL | 1.9849 mL | |
| 25 mM | 0.0635 mL | 0.3176 mL | 0.6352 mL | 1.5880 mL | |
| 30 mM | 0.0529 mL | 0.2647 mL | 0.5293 mL | 1.3233 mL | |
| 40 mM | 0.0397 mL | 0.1985 mL | 0.3970 mL | 0.9925 mL | |
| 50 mM | 0.0318 mL | 0.1588 mL | 0.3176 mL | 0.7940 mL | |
| 60 mM | 0.0265 mL | 0.1323 mL | 0.2647 mL | 0.6616 mL | |
| 80 mM | 0.0198 mL | 0.0992 mL | 0.1985 mL | 0.4962 mL | |
| 100 mM | 0.0159 mL | 0.0794 mL | 0.1588 mL | 0.3970 mL |
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