H3 receptor Selective Inhibitors | Antagonists

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S5926 Pitolisant hydrochloride

Pitolisant (Tiprolisant, BF-2649) acts as a high-affinity competitive antagonist (Ki=0.16 nM) and as an inverse agonist (EC50=1.5 nM) at the human histamine H3 receptor subtype.

Selective H3 receptor, Ki: 0.16 nM
S2813 Ciproxifan Maleate

Ciproxifan (FUB 359) is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes.

Selective Histamine H3 receptor, IC50: 9.2 nM
S8598 S 38093

S 38093 is a histamine H3 antagonist/inverse agonist with a moderate affinity for rat, mouse and human H3 receptors (Ki = 8.8, 1.44 and 1.2 μM, respectively) and no affinity for other histaminergic receptors.

Selective human H3 receptor, Ki: 1.2 μM; rat H3 receptor, Ki: 8.8 μM; mouse H3 receptor, Ki: 1.44 μM
S3176 Betahistine 2HCl

Betahistine (PT-9) is a histamine H3 receptor inhibitor with IC50 of 1.9 μM.

Selective Histamine H3 receptor, IC50: 1.9 μM