LUF6096
Based on 1 Customer Validation
LUF6096, a potent allosteric enhancer of the adenosine A3 receptor, is able to allosterically enhance agonist binding. LUF6096 shows low orthosteric affinity for any of the adenosine receptors. LUF6096 shows protective effects in myocardial ischemia/reperfusion injury.
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- Pureté: 99.16%
- CAS No.: 1116652-18-6
- Formule: C22H21Cl2N3O
- Masse moléculaire:414.33
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Voir tous les produits spécifiques à Isoform Adenosine Receptor
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Activité biologique
adenosine A3 receptor[1]
LUF6096 (10 μM; 30-120 min) decreases the dissociation rate of 125I-AB-MECA from the A3 receptor by 2.5 times in CHO cell membranes[1].
LUF6096 (10 μM; pretreated for 15 min) significantly and dramatically enhances the intrinsic activity of Cl-IB-MECA for the inhibition of the forskolin-stimulated cAMP production in CHO cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult mongrel dogs (15-25 kg) were subjected left anterior descending (LAD) coronary artery occlusion and reperfusion[1]
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Dosage:Twice i.v. bolus for 0.5 mg/kg or single i.v. bolus for 1 mg/kg
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Administration:I.v. bolus
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Result:Produced a marked reduction in infarct size (∼50% reduction) compared with vehicle-treated dogs.
Chemical Information
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CAS No. 1116652-18-6
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Appearance Solid
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Masse moléculaire 414.33
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Formule C22H21Cl2N3O
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Color White to pink
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SMILES
O=C(NC1=CC(NC2=CC=C(Cl)C(Cl)=C2)=NC3=CC=CC=C31)C4CCCCC4
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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
DMSO : 20 mg/mL (48.27 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.
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.
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 (277 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)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Heitman LH, et, al. A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor. J Med Chem. 2009 Feb 26;52(4):926-31. [Content Brief]
[2]. Du L, et, al. Protection from myocardial ischemia/reperfusion injury by a positive allosteric modulator of the A₃ adenosine receptor. J Pharmacol Exp Ther. 2012 Jan;340(1):210-7. [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 | 2.4135 mL | 12.0677 mL | 24.1354 mL | 60.3384 mL |
| 5 mM | 0.4827 mL | 2.4135 mL | 4.8271 mL | 12.0677 mL | |
| 10 mM | 0.2414 mL | 1.2068 mL | 2.4135 mL | 6.0338 mL | |
| 15 mM | 0.1609 mL | 0.8045 mL | 1.6090 mL | 4.0226 mL | |
| 20 mM | 0.1207 mL | 0.6034 mL | 1.2068 mL | 3.0169 mL | |
| 25 mM | 0.0965 mL | 0.4827 mL | 0.9654 mL | 2.4135 mL | |
| 30 mM | 0.0805 mL | 0.4023 mL | 0.8045 mL | 2.0113 mL | |
| 40 mM | 0.0603 mL | 0.3017 mL | 0.6034 mL | 1.5085 mL |
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