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Merck
CN

I7000000

伊曲康唑

European Pharmacopoeia (EP) Reference Standard

别名:

R51211, 奥立康唑, 孢粉

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关于此项目

经验公式(希尔记法):
C35H38Cl2N8O4
化学文摘社编号:
分子量:
705.63
NACRES:
NA.24
PubChem Substance ID:
UNSPSC Code:
41116107
MDL number:
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产品名称

伊曲康唑, European Pharmacopoeia (EP) Reference Standard

InChI

1S/C35H38Cl2N8O4/c1-3-25(2)45-34(46)44(24-40-45)29-7-5-27(6-8-29)41-14-16-42(17-15-41)28-9-11-30(12-10-28)47-19-31-20-48-35(49-31,21-43-23-38-22-39-43)32-13-4-26(36)18-33(32)37/h4-13,18,22-25,31H,3,14-17,19-21H2,1-2H3

SMILES string

CCC(C)N1N=CN(C1=O)c2ccc(cc2)N3CCN(CC3)c4ccc(OCC5COC(Cn6cncn6)(O5)c7ccc(Cl)cc7Cl)cc4

InChI key

VHVPQPYKVGDNFY-UHFFFAOYSA-N

grade

pharmaceutical primary standard

API family

itraconazole

manufacturer/tradename

EDQM

application(s)

pharmaceutical (small molecule)

format

neat

storage temp.

2-8°C

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Biochem/physiol Actions

伊曲康唑抑制细胞色素 P-450 依赖性酶,从而抑制麦角固醇的合成。它通过与 14-α 脱甲基酶相互作用来实现该抑制作用,14-α 脱甲基酶是将羊毛甾醇转化为麦角固醇所必需的细胞色素 P-450 酶。麦角固醇是真菌细胞膜的重要组成部分。因此,它的抑制作用导致细胞通透性增加,造成细胞内容物外泄。伊曲康唑还可能抑制内源性呼吸、与膜磷脂相互作用、抑制酵母转化为菌丝体形式、抑制嘌呤摄取,并减少甘油三酸酯和磷脂的生物合成。
合成广谱三唑类抗真菌药。作用方式:抑制细胞色素 P450 依赖性酶,包括 14α-脱甲基酶。抑制作用导致麦角固醇(一种重要的真菌细胞壁成分)的生物合成受到阻止。

Application

Itraconazole EP Reference standard, intended for use in laboratory tests only as specifically prescribed in the European Pharmacopoeia.

General description

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.For further information and support please go to the website of the issuing Pharmacopoeia.

Other Notes

Sales restrictions may apply.

Packaging

The product is delivered as supplied by the issuing Pharmacopoeia. For the current unit quantity, please visit the EDQM reference substance catalogue.

pictograms

Exclamation mark

signalword

Warning

Hazard Classifications

Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

target_organs

Respiratory system

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Ji-Qin Wu et al.
Antimicrobial agents and chemotherapy, 58(8), 4464-4469 (2014-05-29)
Amphotericin B (AMB) has been a mainstay therapy for fungal infections of the central nervous system, but its use has been limited by its poor penetration into the brain, the mechanism of which remains unclear. In this study, we aimed
A O S Fonseca et al.
The Journal of antimicrobial chemotherapy, 69(6), 1564-1567 (2014-02-14)
The purpose of this study was to compare the in vitro susceptibilities of 22 Brazilian isolates of Pythium insidiosum to antifungals using a standardized inoculum of zoospores and a proposed novel inoculum prepared from cultured mycelia (hyphae) of P. insidiosum.
Zsombor K Nagy et al.
International journal of pharmaceutics, 480(1-2), 137-142 (2015-01-18)
High speed electrospinning (HSES), compatible with pharmaceutical industry, was used to demonstrate the viability of the preparation of drug-loaded polymer nanofibers with radically higher productivity than the known single-needle electrospinning (SNES) setup. Poorly water-soluble itraconazole (ITRA) was formulated with PVPVA64
Jodi Lestner et al.
Expert opinion on drug metabolism & toxicology, 9(7), 911-926 (2013-05-07)
Fungal infections are a major source of global morbidity and mortality. Itraconazole is a triazole antifungal agent that is widely used for the prevention and treatment of fungal infection. While newer antifungal agents are now available, itraconazole is an orally
Ritesh Agarwal et al.
Mycoses, 56(5), 559-570 (2013-03-19)
Patients with aspergilloma can be safely managed with supportive therapy in absence of massive haemoptysis. We hypothesised that chronic cavitary pulmonary aspergillosis (CCPA) could also be managed on similar grounds. The aim of this prospective, randomised controlled trial was to

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