LUF 5834

Potent adenosine A2A and A2B receptor partial agonist CAS# 333962-91-7

LUF 5834

Catalog No. BCC6237----Order now to get a substantial discount!

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LUF 5834: 5mg $127 In Stock
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Chemical structure

LUF 5834

3D structure

Chemical Properties of LUF 5834

Cas No. 333962-91-7 SDF Download SDF
PubChem ID 10066330 Appearance Powder
Formula C17H12N6OS M.Wt 348.38
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO
Chemical Name 2-amino-6-(1H-imidazol-2-ylmethylsulfanyl)-4-(4-oxocyclohexa-2,5-dien-1-ylidene)-1H-pyridine-3,5-dicarbonitrile
SMILES C1=CC(=O)C=CC1=C2C(=C(NC(=C2C#N)SCC3=NC=CN3)N)C#N
Standard InChIKey LOLJUQOCQBYBGT-UHFFFAOYSA-N
Standard InChI InChI=1S/C17H12N6OS/c18-7-12-15(10-1-3-11(24)4-2-10)13(8-19)17(23-16(12)20)25-9-14-21-5-6-22-14/h1-6,23H,9,20H2,(H,21,22)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of LUF 5834

DescriptionPotent A2A and A2B adenosine receptor partial agonist ( Ki = 2.6 nM and EC50 = 12 nM respectively). Also exhibits selectivity for A1 over A3 (Ki values are 2.6 and 538 nM respectively).

LUF 5834 Dilution Calculator

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LUF 5834 Molarity Calculator

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Preparing Stock Solutions of LUF 5834

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.8704 mL 14.3521 mL 28.7043 mL 57.4086 mL 71.7607 mL
5 mM 0.5741 mL 2.8704 mL 5.7409 mL 11.4817 mL 14.3521 mL
10 mM 0.287 mL 1.4352 mL 2.8704 mL 5.7409 mL 7.1761 mL
50 mM 0.0574 mL 0.287 mL 0.5741 mL 1.1482 mL 1.4352 mL
100 mM 0.0287 mL 0.1435 mL 0.287 mL 0.5741 mL 0.7176 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on LUF 5834

A novel nonribose agonist, LUF5834, engages residues that are distinct from those of adenosine-like ligands to activate the adenosine A(2a) receptor.[Pubmed:22188926]

Mol Pharmacol. 2012 Mar;81(3):475-87.

The recent publication of both the antagonist- and agonist-bound structures of the adenosine A(2A) receptor have revealed much about how a ligand may bind to a receptor and cause the conformational changes associated with agonist-mediated activation. In particular, the agonist-bound structure revealed key interactions between the ribose group of adenosine-derived agonists and amino acids in the receptor binding pocket that lead to receptor activation. However, agonists without a ribose group also exist, and we wondered whether such compounds occupy the same agonist binding site. Therefore we used a mutagenesis approach in this study to investigate the mode of binding of 2-amino-4-(4-hydroxyphenyl)- 6-(1H-imidazol-2-ylmethylsulfanyl)pyridine-3,5-dicarbonitrile (LUF5834), a potent partial agonist without a ribose moiety, compared with the adenosine-derived reference agonist 2-[p-(2-carboxyethyl)phenyl-ethylamino]-5'-N-ethylcarboxamidoadenosine (CGS21680). Mutation of the orthosteric residue Phe168 to alanine abrogated the function of both agonists. However, mutation to alanine of residues Thr88 and Ser277 shown by the crystal structures to interact with the ribose group of adenosine-like ligands had no effect on the potency of LUF5834. Furthermore, alanine mutation of Asn253, which makes a hydrogen-bonding interaction with the exocyclic nitrogen of the adenine ring, had minimal effect on LUF5834 affinity but removed agonist activity of this ligand. Mutation of other residues, such as the highly conserved Trp246 or Glu13, had significant deleterious effects on the function of CGS21680 but little effect on LUF5834. In summary, our findings suggest that this class of agonist interacts with distinct residues to activate the receptor compared with classic adenosine derived agonists.

New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine.[Pubmed:15239649]

J Med Chem. 2004 Jul 15;47(15):3707-9.

The adenosine A(2B) receptor is the least well characterized of the four known adenosine receptor subtypes because of the absence of potent, selective agonists. Here, we present five non-adenosine agonists. Among them, 2-amino-4-(4-hydroxyphenyl)-6-(1H-imidazol-2-ylmethylsulfanyl)pyridine-3,5-dicarb onitrile, 17, LUF5834, is a high-efficacy partial agonist with EC(50) = 12 nM and 45-fold selectivity over the adenosine A(3) receptor but lacking selectivity versus the A(1) and A(2A) subtypes. Compound 18, LUF5835, the 3-hydroxyphenyl analogue, is a full agonist with EC(50) = 10 nM.

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