CAS:328541-79-3GlyH-101

GlyH-101, a glycinyl hydrazone compound, is a reversible and voltage-dependent CFTR chloride channel blocker with Ki of 4.3 μM.

规格	价格	促销价格	库存

18817579266

立即询价

咨询

18817579266

立即询价

实验数据

技术信息

CAS号

328541-79-3

储存条件

分子式

C19H15Br2N3O3

运输

蓝冰

分子量

493.15

别名

溶解度

动物实验配方

生物活性

靶点 CFTR (G551D)

EC50:100nM CFTR (F508del)

EC50:25nM
描述The cystic fibrosis transmembrane conductance regulator (CFTR) protein is a cAMP-activated epithelial Cl^- channel. GlyH-101 is a glycine hydrazide compound that inhibits CFTR with a K_i value of 4.3±0.9μM. The inhibitory potency of GlyH-101 against CFTR was reduced at more negative voltages, with K_i values of 1.4, 3.8, 5.0, and 5.6μM for voltages of +60, +20, −20, and −60mV, respectively.^[3] GlyH-101 inhibited cAMP/PKA-activated Cl^- current in a dose- and voltage-dependent manner with IC50 values of 0.3±1.5 and 5.1±1.3μM at +100 and −100mV, respectively.^[4] GlyH-101 at a dosage of 10μM rapidly and reversibly inhibited forskolin-induced hyperpolarization in nasal potential differences in mice (CD1 strain).^[3]
作用机制The inhibition of CFTR by GlyH-101 involves direct CFTR pore occlusion at a site at or near the extracellular-facing pore surface.^[3]

靶点	Description	IC50
CFTR (G551D)		EC50:100nM
CFTR (F508del)		EC50:25nM