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Merck
CN

K1003

酮康唑

99.0-101.0% (EP, titration)

别名:

(±)-顺-1-乙酰基-4-(4-[(2-[2,4-二氯苯基]-2-[1H-咪唑-1-基甲基]-1,3-二氧戊环-4-基)-甲氧基]苯基)哌嗪

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关于此项目

经验公式（希尔记法）:
C26H28Cl2N4O4
化学文摘社编号:
65277-42-1
分子量:
531.43
NACRES:
NA.85
PubChem Substance ID:
24278176
UNSPSC Code:
51101500
EC Number:
265-667-4
MDL number:
MFCD00058579

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产品名称

酮康唑, 99.0-101.0% (EP, titration)

InChI key

XMAYWYJOQHXEEK-OZXSUGGESA-N

InChI

1S/C26H28Cl2N4O4/c1-19(33)31-10-12-32(13-11-31)21-3-5-22(6-4-21)34-15-23-16-35-26(36-23,17-30-9-8-29-18-30)24-7-2-20(27)14-25(24)28/h2-9,14,18,23H,10-13,15-17H2,1H3/t23-,26-/m0/s1

SMILES string

CC(=O)N1CCN(CC1)c2ccc(OC[C@H]3CO[C@@](Cn4ccnc4)(O3)c5ccc(Cl)cc5Cl)cc2

description

Specific Optical Rotation (EP): (−0.10) ∼ +0.10 °

assay

99.0-101.0% (EP, titration)

form

powder

color

white to off-white

antibiotic activity spectrum

Gram-positive bacteria
fungi
yeast

mode of action

enzyme | inhibits

storage temp.

2-8°C

Quality Level

200

Gene Information

human ... ABCB1(5243), CYP11B1(1584), CYP11B2(1585), CYP17A1(1586), CYP19A1(1588), CYP1A2(1544), CYP24A1(1591), CYP26A1(1592), CYP3A4(1576), CYP51A1(1595), KCNH1(3756)
mouse ... Abcb1a(18671), Abcb1b(18669)
rat ... Alox5(25290), Cyp17a1(25146), Cyp51(25427), Cyp7a1(25428)

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相关类别

Application

CYP3A4抑制剂
酮康唑是一种广谱抗真菌药，可用于治疗念珠菌病、慢性粘膜皮肤念珠菌病、口腔鹅口疮、念珠菌、芽生菌病、球孢子菌病、组织胞浆菌病、色素霉菌病和副球菌病。 它被用于鉴定猴模型中p-糖蛋白/CYP3A限制的生物利用度，研究白细胞介素1介导的抗肿瘤作用以及 体内药物相互作用

Biochem/physiol Actions

抗真菌剂
酮康唑能够与14-α去甲基化酶发生相互作用，这是一种细胞色素P-450酶，是羊毛甾醇转化为麦角甾醇所必需的酶。这种相互作用抑制了麦角甾醇合成并导致真菌细胞渗透性增强。其他可能的作用机制是抑制内源性呼吸、与膜磷脂的相互作用、抑制酵母转化为菌丝体形式、抑制嘌呤摄取以及破坏甘油三酯和/或磷脂生物合成。酮康唑可抑制血栓素和甾醇的合成，如醛固酮、皮质醇和睾酮。

General description

化学结构：咪唑

signalword

Danger

Hazard Classifications

Acute Tox. 3 Oral - Aquatic Acute 1 - Aquatic Chronic 1 - Repr. 1B - STOT RE 2

存储类别

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000506796
0000506796
0000478500
0000478500
0000403452

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The Journal of pharmacology and experimental therapeutics, 268(3), 1278-1283 (1994-03-01)
Biotransformation of the tricyclic antidepressant desipramine (DMI) to its metabolite 2-hydroxy-desipramine (2-OH-DMI) was studied in vitro using microsomal preparations from human, monkey, mouse and rat liver. In all species 2-OH-DMI was the principal identified metabolite. Mean (+/- S.E.) reaction parameters
Keith W Ward et al.
Drug metabolism and disposition: the biological fate of chemicals, 32(2), 172-177 (2004-01-28)
The effect of P-glycoprotein (Pgp) and/or CYP3A on the disposition of xenobiotics has been extensively investigated and is often of interest during drug discovery lead optimization. We have previously described a monkey pharmacokinetic screen to rapidly estimate absorption and first-pass
Flor Soriano-Agatón et al.
Journal of natural products, 68(11), 1581-1587 (2005-11-29)
Zanthoxylum chiloperone var. angustifolium was investigated. Alkaloids 1-3 from the canthin-6-one series were characterized. Derivatives 7-28 were prepared by hemisynthesis or total synthesis. All compounds were tested for in vitro antifungal activities against five pathogenic fungal strains. Analogues of canthin-6-one
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Cancer research, 50(15), 4709-4717 (1990-08-01)
In the present studies, the regulatory role of adrenal hormones on the antitumor activity of recombinant human interleukin 1 alpha (IL-1 alpha) was investigated. Ketoconazole, a potent but transient inhibitor of adrenal steroid hormone biosynthesis, inhibited IL-1 alpha induced increases
Sarah Tsao et al.
Antimicrobial agents and chemotherapy, 53(4), 1344-1352 (2009-02-19)
Candida albicans frequently develops resistance to treatment with azole drugs due to the acquisition of gain-of-function mutations in the transcription factor Tac1p. Tac1p hyperactivation in azole-resistant isolates results in the constitutive overexpression of several genes, including CDR1 and CDR2, which
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