333962-91-7
Chemical Structure
LUF5834
- CAS No.: 333962-91-7
- Formula:C17H12N6OS
- Molecular Weight:348.38
IUPAC Name: 2-(((1H-imidazol-2-yl)methyl)thio)-6-amino-4-(4-hydroxyphenyl)pyridine-3,5-dicarbonitrile
InChIKey: OFHKDLYFKPBXER-UHFFFAOYSA-N
SMILES: N#CC1=C(C2=CC=C(O)C=C2)C(C#N)=C(SCC3=NC=CN3)N=C1N
Biological Activity: 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[1][2][3][4][5].
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LUF5834 | 99.8% | 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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References
- [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.
