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
EC 号:
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
产品名称
克霉唑,
表单
powder
质量水平
抗生素抗菌谱
fungi
作用机制
cell membrane | interferes
protein synthesis | interferes
创始人
Schering Plough
SMILES字符串
Clc1ccccc1C(c2ccccc2)(c3ccccc3)n4ccnc4
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
InChI key
VNFPBHJOKIVQEB-UHFFFAOYSA-N
基因信息
human ... ABCB1(5243), CYP17A1(1586), CYP3A4(1576)
mouse ... Abcb1a(18671), Abcb1b(18669)
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一般描述
化学结构：咪唑
应用
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
生化/生理作用
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。
特点和优势
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。
警示用语：
Warning
危险分类
Acute Tox. 4 Oral - Aquatic Acute 1 - Aquatic Chronic 1 - Eye Irrit. 2 - Skin Irrit. 2
储存分类代码
11 - Combustible Solids
WGK
WGK 3
个人防护装备
dust mask type N95 (US), Eyeshields, Gloves
K W Henry et al.
Antimicrobial agents and chemotherapy, 44(10), 2693-2700 (2000-09-19)
Infections due to Candida albicans are usually treated with azole antifungals such as fluconazole, but treatment failure is not uncommon especially in immunocompromised individuals. Relatedly, in vitro studies demonstrate that azoles are nonfungicidal, with continued growth at strain-dependent rates even
Martindale: The Extra Pharmacopoeia, 403-403 (1996)
Monica Kam Draskau et al.
Toxicology and applied pharmacology, 422, 115554-115554 (2021-04-29)
Clotrimazole is a non-prescription and broad-spectrum antifungal drug sold under brand names such as Canesten® and Lotrimin®. It is used to treat different types of fungal infections, from oral thrush to athlete's foot and vaginal mycosis. The level of exposure
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
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
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