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Merck
CN

SML2287

泊沙康唑标准液

≥98% (HPLC), lanosterol 14α-demethylase inhibitor, powder

别名:

泊沙康唑标准液 溶液, 2,5-脱水-1,3,4-丁氧基-2-C-(2,4-二氟苯基)-4-[[4-[4-[4-[1-[(1S,2S)-1-]乙基-2-羟丙基] -1,5-二氢-5-氧代-4H-1,2,4-三唑-4-基]苯基] -1-哌嗪基]苯氧基]甲基] -1-(1H-1, 2,4-三唑-1-基)-D-苏糖醇, Sch 56592

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关于此项目

经验公式(希尔记法):
C37H42F2N8O4
化学文摘社编号:
分子量:
700.78
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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产品名称

泊沙康唑标准液, ≥98% (HPLC)

SMILES string

Fc1c(ccc(c1)F)[C@@]3(OC[C@H](C3)COc4ccc(cc4)N5CCN(CC5)c6ccc(cc6)N7C=NN(C7=O)[C@H]([C@@H](O)C)CC)C[n]2ncnc2

InChI

1S/C37H42F2N8O4/c1-3-35(26(2)48)47-36(49)46(25-42-47)31-7-5-29(6-8-31)43-14-16-44(17-15-43)30-9-11-32(12-10-30)50-20-27-19-37(51-21-27,22-45-24-40-23-41-45)33-13-4-28(38)18-34(33)39/h4-13,18,23-27,35,48H,3,14-17,19-22H2,1-2H3/t26-,27+,35-,37-/m0/s1

InChI key

RAGOYPUPXAKGKH-XAKZXMRKSA-N

assay

≥98% (HPLC)

form

powder

optical activity

[α]/D -24 to -32°, c = 1.0 in chloroform-d

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

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Application

泊沙康唑用于:
  • 土曲霉抗真菌药敏试验
  • 作为羊毛甾醇14α-脱甲基酶 (CYP51) 特异性抑制剂,研究其对白色念珠菌细胞膜通透性的影响
  • 研究其对前鞭毛体的影响

Biochem/physiol Actions

泊沙康唑是一种高效的广谱抗真菌剂,可抑制念珠菌引起的酵母菌感染。它通过抑制羊毛甾醇14α-脱甲基酶 (CYP51)阻断真菌生长。与其他抗真菌唑类药物相反,泊沙康唑据报道不会诱导外排泵机制。泊沙康唑对各类南美锥虫病的病原体克氏锥虫菌株具有抑制作用。

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Eleftheria Mavridou et al.
Antimicrobial agents and chemotherapy, 54(2), 860-865 (2009-11-18)
The in vivo efficacy of posaconazole against 4 clinical Aspergillus fumigatus isolates with posaconazole MICs ranging from 0.03 to 16 mg/liter, as determined by CLSI method M38A, was assessed in a nonneutropenic murine model of disseminated aspergillosis. The underlying resistance
Yanjun Li et al.
Clinical pharmacokinetics, 49(6), 379-396 (2010-05-21)
Posaconazole is a recently approved lipophilic triazole antifungal agent that exhibits potent and broad-spectrum antifungal activity in vitro and in vivo against most Candida spp., Cryptococcus neoformans, Aspergillus spp., many Zygomycetes, endemic fungi and dermatophytes. It has been documented that
Harrys A Torres et al.
The Lancet. Infectious diseases, 5(12), 775-785 (2005-11-29)
Posaconazale is a new triazole drug being investigated in phase III clinical trials for the treatment and prevention of invasive fungal infections. In-vitro and in-vivo studies showed that posaconazole has broad-spectrum activity against most Candida species, Cryptococcus neoformans, Aspergillus species
Laura Judith Marcos-Zambrano et al.
Antimicrobial agents and chemotherapy, 61(7) (2017-04-26)
The objectives of our study were to describe the characteristics of patients with Candida guilliermondii candidemia and to perform an in-depth microbiological characterization of isolates and compare them with those of patients with C. albicans candidemia. We described the risk
Galina I Lepesheva et al.
The Journal of biological chemistry, 285(33), 25582-25590 (2010-06-10)
Trypanosoma cruzi causes Chagas disease (American trypanosomiasis), which threatens the lives of millions of people and remains incurable in its chronic stage. The antifungal drug posaconazole that blocks sterol biosynthesis in the parasite is the only compound entering clinical trials

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