DPTN dihydrochloride

• CAT Number: I041179
• CAS Number: 325767-87-1
• Molecular Formula: C22H20Cl2N4OS
• Molecular Weight: 459.39
• Purity: ≥95%
• Synonyms: N-[4-(3,5-dimethylphenyl)-5-pyridin-4-yl-1,3-thiazol-2-yl]pyridine-3-carboxamide;dihydrochloride
• InChI: InChI=1S/C22H18N4OS.2ClH/c1-14-10-15(2)12-18(11-14)19-20(16-5-8-23-9-6-16)28-22(25-19)26-21(27)17-4-3-7-24-13-17;;/h3-13H,1-2H3,(H,25,26,27);2*1H
• InChIKey: GTWKWBXTCBUKTR-UHFFFAOYSA-N
• SMILES: CC1=CC(=CC(=C1)C2=C(SC(=N2)NC(=O)C3=CN=CC=C3)C4=CC=NC=C4)C.Cl.Cl

DPTN is a potent and selective human, mouse, and rat A3AR antagonist with Ki values of 1.65, 9.61, and 8.53 nM, respectively[1].
DPTN is indeed a potent antagonist for human, mouse, and rat A3ARs . DPTN is weaker at mouse and rat compared with human A3AR and has reduced selectivity (about 20-fold vs A2BAR).[1].
The Binding affinity of BNPT (10 μM) is tested in membranes of transfected HEK293 cells, the Ki values are 162 ± 49, 121 ± 42, 230 ± 40, and 1.65 ± 0.57 nM for hA1, hA2A, hA2B, and hA3, respectively[1].
DPTN’s Ki values at respective A1, A2A, A2B, and A3 receptors are 411, 830, 189, and 9.61 nM (mouse); and 333, 1147, 163, and 8.53 nM (rat) [1].

Reference

[1]. Zhan-Guo Gao, et al. Pharmacological characterization of DPTN and other selective A3 adenosine receptor antagonist. Purinergic Signal. 2021 Dec;17(4):737-746.
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