GlyH-101 是一种可渗透入细胞的CFTR阻断剂，Ki为1.4 uM。
产品描述
GlyH-101 is a cell-permeable glycinyl hydrazone compound that blocks CFTR with Ki of 1.4 uM.
体外活性
GlyH-101 reversibly inhibits CFTR Cl- conductance in<1 min. [1] In rabbit isolated ventricular myocytes, GlyH-101 also blocks cardiac I(Cl.PKA) channels. [2] In transfected FRT (SLC26A9-FRT) cells, GlyH-101 inhibits SLC26A9-mediated Cl- currents. [3]
体内活性
In mice, Topical GlyH-101 (10 μM) in mice rapidly and reversibly inhibits forskolin-induced hyperpolarization in nasal potential differences. In a cholera model, intraluminal GlyH-101 (2.5 μg) reduces cholera toxin-induced intestinal fluid secretion by approximately 80%.[1]
Cas No.
328541-79-3
分子式
C19H15Br2N3O3
分子量
493.155
别名
GlyH 101
储存和溶解度
DMSO:49.3 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
