glyh-101

Description: GlyH-101 is a novel and potent CFTR inhibitor (cystic fibrosis transmembrane conductance regulator) with Ki of 1.4 uM. GlyH-101 is a glycine hydrazide that has been shown to block CFTR channels. GlyH-101 blocked I(Cl.PKA) in a concentration- and voltage-dependent fashion (IC(50) at +100 mV=0.3 A+/- 1.5 uM and at -100 mV=5.1 A+/- 1.3 uM). GlyH-101 blocks the open pore of cardiac CFTR channels at an electrical distance of 0.15 A+/- 0.03 from the external membrane surface.

References: Melis N, Tauc M, Cougnon M, Bendahhou S, Giuliano S, Rubera I, Duranton C. Revisiting CFTR inhibition: a comparative study of CFTRinh -172 and GlyH-101 inhibitors. Br J Pharmacol. 2014 Aug; 171(15):3716-27.