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Antifungal agent 22
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Antifungal agent 22图片
CAS NO:2640054-39-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
Antifungal agent 22 (compound D16) 是一种潜在的口服有效的抗真菌药物,其IC50值为 0.5 μg/mL。Antifungal agent 22 能穿透血脑屏障,通过破坏真菌细胞膜的完整性杀死C. neoformansH99 细胞。Antifungal agent 22 具有选择性抗隐球菌活性,代谢稳定性好,细胞毒性低。
生物活性

Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with anIC50of 0.5 μg/mL. Antifungal agent 22 can penetrate the blood-brain barrier and kill theC. neoformansH99 cells by destroying the integrity offungalcell membranes. Antifungal agent 22 shows selective anti-Cryptococcusactivity with good metabolic stability and low cytotoxicity[1].

IC50& Target

IC50: 0.5 μg/mL (Fungal)[1].

体外研究
(In Vitro)

Antifungal agent 22 (compound D16) (0-1 μg/mL, 24 h) inhibits ergosterol biosynthesis, which results in stress-induced upregulation of ERG genes inC. neoformansH99[1].
Antifungal agent 22 (0-8 μg/mL) effectively inhibits the growth ofC. neoformansH99 (0-72 h), inhibits the formation ofC. neoformansH99 biofilms in a concentration-dependent manner (24 h)[1].
Antifungal agent 22 (0-8 μg/mL, 48-72 h) shows selective anti-Cryptococcusactivity, has a fungistatic effect[1].
Antifungal agent 22 (0-100 μM, 48 h) shows low cytotoxicity against a human HUVEC cell line with an IC50of 20.18 μM[1].

Cell Proliferation Assay

Cell Line:C. neoformansH99 cells[1]
Concentration:0, 1, 2, 4, 8 μg/mL
Incubation Time:0, 4, 8, 12, 24, 48, and 72 h
Result:Almost completely inhibited the growth ofC. neoformansH99 at 8 μg/mL, remained at nearly 100% inhibition rate after 72 h, had minimum fungicidal concentrations of 8 μg/mL.

Cell Viability Assay

Cell Line:Fungal cells (RPMI 1640 medium)[1]
Concentration:0, 0.5, 1, 2, 4, 8 μg/mL
Incubation Time:48, 72 h
Result:Showed selective anti-Cryptococcusactivity, withIC50range of 0.06-2 μg/mL and aMIC50value (averageIC50values) of 0.62 μg/mL.
体内研究
(In Vivo)

Antifungal agent 22 (D16) (15 mg/kg, Intragastrically, daily for 5 days) shows potent anti-Cryptococcalefficacy[1].

Animal Model:ICR female mice (18-22 g, 4-6 weeks, tail vein injected withC. neoformansH99 cells)[1]
Dosage:15 mg/kg
Administration:Intragastrically, daily for 5 days
Result:Showed potent anti-Cryptococcalefficacy, significantly reduced the number ofC. neoformansH99 cells in the brain after 5 days, prolong the median survival time (14 days) of the infected mice at a dose of 15 mg/kg.
分子量

446.86

Formula

C21H26Cl3NOS

CAS 号

2640054-39-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.