Art. -Nr.: HY-103170

LUF5834

Name: LUF5834
Brand: MedChemExpress
SKU: HY-103170
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LUF5834 is a selective A_2A/A_2B adenosine receptor agonist. LUF5834 stabilizes the S₃ intermediate active conformation of A_2AAR and activates downstream G protein-coupled pathways. LUF5834 activates Gs-coupled A_2A signaling and cAMP, and partially activates A_2B 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 A_2A/A_2B receptor-mediated diseases, such as cardiac ischemia.

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Reinheit : 99.8%
CAS. Nr.: 333962-91-7
Formel: C₁₇H₁₂N₆OS
Molecular Weight:348.38

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

LUF5834 Chemical Structure

CAS. Nr.: 333962-91-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[4]^[2]

A2BR

79.6 nM (Ki)

A2AR

16.2 nM (EC₅₀)

A2AR

21 nM (Kd)

Alle Adenosine Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	12 nM Compound: 17	Agonistic activity against human adenosine A2B receptor expressed in CHO cells Agonistic activity against human adenosine A2B receptor expressed in CHO cells	[PMID: 15239649]

In Vitro

Regulation of Cardiac Pump FunctionOthers

Regulation of Cardiac Pump Function

LUF5834 (10 -100 nM; 12 h) does not reduce necrosis in H9c2 (2-1) cardiomyocytes subjected to simulated ischemia, but when combined with CPA in adenosine deaminase-pretreated H9c2 (2-1) cardiomyocytes, it enhances the cytoprotective effect against simulated ischemia-induced necrosis, and this synergistic effect is abolished by the A_2B antagonist MRS1754 (HY-14121)^[5].

Others

LUF5834 acts as a partial agonist at purified A_2AR-V229C by stabilizing the long-lived S3 active state^[1].
LUF5834 binds to HEK293hA_2AR membranes with a k_on of 1.1 × 10⁷ M^-1·min^-1, a k_off of 0.23 min^-1, a receptor residence time of 4.2 min, and a K_D = 21 nM^[2].
LUF5834 displaces specific [³H]-ZM241385 binding in HEK293hA_2AR membranes with K_i = 16 nM^[2].
LUF5834 acts as a partial agonist in label-free impedance assays in HEK293hA_2AR cells, with an EC₅₀ of 3.6 nM and an E_max of 47%; it stimulates cAMP production in HEK293hA_2AR cells, with an EC₅₀ of 21 nM and an E_max of 50%^[2].
LUF5834 binds to the wild-type A_2A receptor with a K_i of 79.6 nM, and its binding affinity is not reduced by the T88^3.36A or S277^7.42A mutation^[4].
LUF5834 is a high-potency partial agonist of the wild-type A_2A receptor (EC₅₀ 16.2 nM) and retains or gains potency in multiple ribose-interacting mutants, but loses agonist efficacy at N253^6.55A^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[5]

Cell Line:

H9c2(2-1) embryonic rat atrial cardiac cells
Concentration:

10 nM
10 nM, 100 nM (co‑treated with CPA)
Incubation Time:

12 h
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 A_2B antagonist MRS1754.

Chemical Information

CAS. Nr. 333962-91-7
Appearance Solid
Molecular Weight 348.38
Formel C₁₇H₁₂N₆OS
Color White to light yellow
SMILES

N#CC1=C(C2=CC=C(O)C=C2)C(C#N)=C(SCC3=NC=CN3)N=C1N
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8704 mL

14.3521 mL

28.7043 mL

5 mM

0.5741 mL

2.8704 mL

5.7409 mL

10 mM

0.2870 mL

1.4352 mL

2.8704 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Ye L, et al. Activation of the A2A adenosine G-protein-coupled receptor by conformational selection. Nature. 2016 May 12;533(7602):265-8.

[2]. Guo D, et al. Functional efficacy of adenosine A₂A receptor agonists is positively correlated to their receptor residence time. British journal of pharmacology. 2012 Jul;166(6):1846-59.

[3]. Wolska N, et al. Blood Platelet Adenosine Receptors as Potential Targets for Anti-Platelet Therapy. International journal of molecular sciences. 2019 Nov 03;20(21):5475.

[4]. Lane JR, et al. A novel nonribose agonist, LUF5834, engages residues that are distinct from those of adenosine-like ligands to activate the adenosine A(2a) receptor. Molecular pharmacology. 2012 Mar;81(3):475-87. [Content Brief]

[5]. Urmaliya VB, et al. Cardioprotection induced by adenosine A1 receptor agonists in a cardiac cell ischemia model involves cooperative activation of adenosine A2A and A2B receptors by endogenous adenosine. Journal of cardiovascular pharmacology. 2009 May;53(5):424-33.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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LUF5834

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