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GlyH-101

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Chemical Structure| 328541-79-3 同义名 : CFTR Inhibitor II;Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor II
CAS号 : 328541-79-3
货号 : A128948
分子式 : C19H15Br2N3O3
纯度 : 99%+
分子量 : 493.149
MDL号 : MFCD01532954
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 55 mg/mL(111.53 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • CFTR

    CFTR, Ki:4.3 μM
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 Ki value of 4.3±0.9μM. The inhibitory potency of GlyH-101 against CFTR was reduced at more negative voltages, with Ki 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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.14mL

2.03mL

1.01mL

20.28mL

4.06mL

2.03mL
参考文献

[1]Mutyam V, Libby EF, et al. Therapeutic benefit observed with the CFTR potentiator, ivacaftor, in a CF patient homozygous for the W1282X CFTR nonsense mutation. J Cyst Fibros. 2017 Jan;16(1):24-29.

[2]Hadida S, Van Goor F,et al. Discovery of N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide(VX-770, ivacaftor), a potent and orally bioavailable CFTR potentiator. J Med Chem. 2014 Dec 11;57(23):9776-95.

[3]Muanprasat C, Sonawane ND, Salinas D, Taddei A, Galietta LJ, Verkman AS. Discovery of glycine hydrazide pore-occluding CFTR inhibitors: mechanism, structure-activity analysis, and in vivo efficacy. J Gen Physiol. 2004;124(2):125-137. doi:10.1085/jgp.200409059

[4]Barman PP, Choisy SC, Gadeberg HC, Hancox JC, James AF. Cardiac ion channel current modulation by the CFTR inhibitor GlyH-101. Biochem Biophys Res Commun. 2011;408(1):12-17. doi:10.1016/j.bbrc.2011.03.089