C6019
克霉唑
98.5-100.5% (dry basis), powder, Ca²⁺-activated K⁺ channels inhibitor
别名:
1-[（2-氯苯基）二苯基甲基]-1-H咪唑, 1-（o-氯-α，α-二苯基苄基）咪唑, 1-（o-氯三苯）咪唑
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关于此项目
经验公式（希尔记法）:
C22H17ClN2
化学文摘社编号:
分子量:
344.84
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
EC Number:
245-764-8
MDL number:
产品名称
克霉唑,
InChI key
VNFPBHJOKIVQEB-UHFFFAOYSA-N
InChI
1S/C22H17ClN2/c23-21-14-8-7-13-20(21)22(25-16-15-24-17-25,18-9-3-1-4-10-18)19-11-5-2-6-12-19/h1-17H
SMILES string
Clc1ccccc1C(c2ccccc2)(c3ccccc3)n4ccnc4
form
powder
antibiotic activity spectrum
fungi
mode of action
cell membrane | interferes
protein synthesis | interferes
originator
Schering Plough
Quality Level
Gene Information
human ... ABCB1(5243), CYP17A1(1586), CYP3A4(1576)
mouse ... Abcb1a(18671), Abcb1b(18669)
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Application
克霉唑已被用于：
- 在假丝酵母中，研究用唑类抗生素处理后，编码唑类靶酶羊毛甾醇脱甲基酶的基因ERG11的上调
- 研究从长期抗真菌治疗的患者中分离的假丝酵母的耐药性的发展
- 通过线粒体应激诱导应激颗粒
- 抑制1-氯-2,4-二硝基苯（CDNB）处理诱导的高密度镰状细胞的体外形成
- 在细胞培养物中抑制细胞色素P450酶
Biochem/physiol Actions
克霉唑是一种Ca2+-活化的K+ 通道的特异性抑制剂。 它是一种抗真菌的唑类。克霉唑是一种咪唑的衍生物，具有与酮康唑相似的抗微生物作用和活性。 它可抑制细胞色素P450依赖性14α -去甲基化酶，这对麦角甾醇生物合成至关重要。累积的14α -甲基化甾醇可改变敏感真菌的膜结构，同时改变细胞膜的通透性。
Features and Benefits
该化合物由Schering Plough开发。要浏览其他药物开发化合物和批准的药物/候选药物列表，单击此处。
General description
化学结构：咪唑
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Aquatic Acute 1 - Aquatic Chronic 1 - Eye Irrit. 2 - Skin Irrit. 2
存储类别
11 - Combustible Solids
wgk
WGK 3
ppe
dust mask type N95 (US), Eyeshields, Gloves
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Antimicrobial agents and chemotherapy, 35(11), 2302-2305 (1991-11-01)
The impact of prolonged antifungal therapy on the development of resistance was examined in 61 patients with oropharyngeal thrush. Fifty-nine patients had symptomatic human immunodeficiency virus infection, one had lung cancer, and one had metastatic prostate cancer. Cultures of pharyngeal
A Shartava et al.
American journal of hematology, 62(1), 19-24 (1999-09-01)
Clotrimazole, a specific inhibitor of the Ca(2+) activated potassium (Gardos) channel, and the antioxidant N-acetylcysteine were found to inhibit the in vitro formation of high-density sickle cells induced by treatment with 1-chloro-2,4-dinitrobenzene (CDNB). The CDNB induced leakage of K(+) can
Nancy Kedersha et al.
The Journal of cell biology, 169(6), 871-884 (2005-06-22)
Stress granules (SGs) are cytoplasmic aggregates of stalled translational preinitiation complexes that accumulate during stress. GW bodies/processing bodies (PBs) are distinct cytoplasmic sites of mRNA degradation. In this study, we show that SGs and PBs are spatially, compositionally, and functionally
B S Jensen et al.
Current drug targets, 2(4), 401-422 (2001-12-06)
This review discusses the Ca2+-activated K+ channels of intermediate conductance (IK channels), and their historical discovery in erythrocytes, their classical biophysical characteristics, physiological function, molecular biology as well as their role as possible molecular targets for pharmacological intervention in various
Martindale: The Extra Pharmacopoeia, 403-403 (1996)
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