Product overview

Name LUF7982
Biological description

Novel, selective A2B covalent ligand (apparent pKi values at A2BARs are 8.10 and 9.17 (after 4h), where a Ki shift indicates a covalent mode of action). Displays ~100 -fold selectivity for A2B compared to A1, A2A and A3 receptors. LUF7982 covalently targets lysine residue(s) on the receptor and binds persistently in radioligand displacement and wash-out assays. LUF7982 allows for novel ways to interrogate the A2BAR.

Sold under license from the Oncode Institute and Universiteit Leiden

Purity >95%
Description

Novel Selective A2B covalent ligand. Binds irreversibly.

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Solubility & Handling

Storage instructions -20°C
Solubility overview Soluble in DMSO
Storage of solutions Prepare and use solutions on the same day if possible. Store solutions at -20°C for up to one month if storage is required. Equilibrate to RT and ensure the solution is precipitate free before use.
Shipping Conditions Stable for ambient temperature shipping. Follow storage instructions on receipt.
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use

Calculators

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Dilution

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Chemical Data

Purity >95%
Chemical name 4-(2,6-dioxo-1-propyl-2,3,6,7-tetrahydro-1H-purin-8-yl)benzenesulfonyl fluoride
Molecular Weight 352.3
Chemical structure  Chemical Structure
Molecular Formula C14H13FN4O4S
SMILES CCCN1C(=O)NC2=C(NC(=N2)C2=CC=C(C=C2)S(F)(=O)=O)C1=O
InChiKey LDROORXQLOXQKW-UHFFFAOYSA-N
Licensing details

Sold under license from the Oncode Cancer Institute and Universiteit Leiden

References for LUF7982

References are publications that support the biological activity of the product
  • Development of subtype-selective covalent ligands for the adenosine A(2B) receptor by tuning the reactive group.

    Beerkens BLH et al (2022) RSC medicinal chemistry 13 : 850-856

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