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Merck
CN

C2992

Sigma-Aldrich

CFTR(inh)-172

≥98% (HPLC), powder

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别名:
5-[(4-羧基苯基)亚甲基]-2-硫氧-3- [(3-三氟甲基)苯基-4-噻唑烷酮
经验公式(希尔记法):
C18H10F3NO3S2
分子量:
409.40
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

质量水平

检测方案

≥98% (HPLC)

形式

powder

颜色

yellow

溶解性

DMSO: ≥10 mg/mL
H2O: insoluble

储存温度

2-8°C

SMILES字符串

OC(=O)c1ccc(cc1)\C=C2\SC(=S)N(C2=O)c3cccc(c3)C(F)(F)F

InChI

1S/C18H10F3NO3S2/c19-18(20,21)12-2-1-3-13(9-12)22-15(23)14(27-17(22)26)8-10-4-6-11(7-5-10)16(24)25/h1-9H,(H,24,25)/b14-8+

InChI key

JIMHYXZZCWVCMI-RIYZIHGNSA-N

相关类别

应用

CFTR(inh)-172用于特异性抑制囊性纤维化跨膜电导调节因子(CFTR)的活性。也可用作 CFTR抑制剂 Inh-172处理福司柯林(毛喉素)和IBMX。

生化/生理作用

CFTR (inh)-172 是囊性纤维化跨膜传导调节因子 (CFTR) 的抑制剂。K i = 300 nM。CFTR (inh)-172 导致快速、可逆和非电压依赖性抑制;为动物止泻药。CTFR (inh)-172 可能是研究霍乱和其他分泌性腹泻囊性纤维化和肠液丢失动物模型的有用工具。CTFR (inh)-172 在结构上与已知的非特异性 CFTR 抑制剂 DPC,NPPB(货号N4779)和格列本脲。

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Electrophysiological evaluation of cystic fibrosis conductance transmembrane regulator (CFTR) expression in human monocytes
Ettorre M, et al.
Biochimica et biophysica acta. General subjects, 1840(10), 3088-3095 (2014)
Defective CFTR expression and function are detectable in blood monocytes: development of a new blood test for cystic fibrosis
Sorio C, et al.
Testing, 6(7), e22212-e22212 (2011)
An unexpected effect of TNF-alpha on F508del-CFTR maturation and function
Bitam S, et al.
F1000Research, 4 (2015)
Jinxue Ruan et al.
Molecular therapy. Nucleic acids, 16, 73-81 (2019-03-11)
Cystic fibrosis (CF) is a lethal autosomal recessive disease caused by mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) gene. Nuclease-mediated precise gene editing (PGE) represents a promising therapy for CF, for which an efficient strategy that is free
Tonghui Ma et al.
The Journal of clinical investigation, 110(11), 1651-1658 (2002-12-05)
Secretory diarrhea is the leading cause of infant death in developing countries and a major cause of morbidity in adults. The cystic fibrosis transmembrane conductance regulator (CFTR) protein is required for fluid secretion in the intestine and airways and, when

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