LUF5834
Based on 1 Customer Validation
LUF5834 is a selective A2A/A2B adenosine receptor agonist. LUF5834 stabilizes the S3 intermediate active conformation of A2AAR and activates downstream G protein-coupled pathways. LUF5834 activates Gs-coupled A2A signaling and cAMP, and partially activates A2B to stimulate cAMP. LUF5834 combined with A1 agonists enhances protective effects in the absence of endogenous adenosine. LUF5834 can be used in research related to A2A/A2B receptor-mediated diseases, such as cardiac ischemia.
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- Pureza : 99.8%
- No. CAS: 333962-91-7
- Fòrmula: C17H12N6OS
- Peso molecular:348.38
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Almacenamiento: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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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
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Actividad biológica
Descripciòn
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A2BR 79.6 nM (Ki) |
A2AR 16.2 nM (EC50) |
A2AR 21 nM (Kd) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
12 nM
Compound: 17
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Agonistic activity against human adenosine A2B receptor expressed in CHO cells
Agonistic activity against human adenosine A2B receptor expressed in CHO cells
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[PMID: 15239649] |
In Vitro
LUF5834 binds to HEK293hA2AR membranes with a kon of 1.1 × 107 M-1·min-1, a koff of 0.23 min-1, a receptor residence time of 4.2 min, and a KD = 21 nM[2].
LUF5834 displaces specific [3H]-ZM241385 binding in HEK293hA2AR membranes with Ki = 16 nM[2].
LUF5834 acts as a partial agonist in label-free impedance assays in HEK293hA2AR cells, with an EC50 of 3.6 nM and an Emax of 47%; it stimulates cAMP production in HEK293hA2AR cells, with an EC50 of 21 nM and an Emax of 50%[2].
LUF5834 binds to the wild-type A2A receptor with a Ki of 79.6 nM, and its binding affinity is not reduced by the T883.36A or S2777.42A mutation[4].
LUF5834 is a high-potency partial agonist of the wild-type A2A receptor (EC50 16.2 nM) and retains or gains potency in multiple ribose-interacting mutants, but loses agonist efficacy at N2536.55A[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H9c2(2-1) embryonic rat atrial cardiac cells
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Concentration:10 nM
10 nM, 100 nM (co‑treated with CPA) -
Incubation Time:12 h
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Result:Showed no significant cytoprotective effect against simulated‑ischemia‑induced necrosis in H9c2(2‑1) cardiomyocytes.
Augmented cytoprotective effect against simulated‑ischemia‑induced necrosis, and this synergistic effect was abolished by A2B antagonist MRS1754.
Chemical Information
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No. CAS 333962-91-7
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Appearance Solid
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Peso molecular 348.38
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Fòrmula C17H12N6OS
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Color White to light yellow
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SMILES
N#CC1=C(C2=CC=C(O)C=C2)C(C#N)=C(SCC3=NC=CN3)N=C1N
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 20 mg/mL (57.41 mM; Need ultrasonic and warming; 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)
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.8704 mL | 14.3521 mL | 28.7043 mL | 71.7607 mL |
| 5 mM | 0.5741 mL | 2.8704 mL | 5.7409 mL | 14.3521 mL | |
| 10 mM | 0.2870 mL | 1.4352 mL | 2.8704 mL | 7.1761 mL | |
| 15 mM | 0.1914 mL | 0.9568 mL | 1.9136 mL | 4.7840 mL | |
| 20 mM | 0.1435 mL | 0.7176 mL | 1.4352 mL | 3.5880 mL | |
| 25 mM | 0.1148 mL | 0.5741 mL | 1.1482 mL | 2.8704 mL | |
| 30 mM | 0.0957 mL | 0.4784 mL | 0.9568 mL | 2.3920 mL | |
| 40 mM | 0.0718 mL | 0.3588 mL | 0.7176 mL | 1.7940 mL | |
| 50 mM | 0.0574 mL | 0.2870 mL | 0.5741 mL | 1.4352 mL |
LUF5834 Related Classifications
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