切换导航

Amphotericin B

现货
Catalog No.
B1885
两亲多烯抗生素
组合的产品项目
规格价格库存 数量
100mg
¥ 530.00
现货
500mg
¥ 930.00
现货
10mM (in 1mL DMSO)
¥ 550.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

Amphotericin B, a polyene antifungal antibiotic, has been produced from a strain of Streptomyces nodosus with an IC50 of 0.028–0.290 μg/ml.

In vitro: Amphotericin B was the most effective drug for treating many life-threatening fungal infections. In cells expressing TLR2 and CD14, amphotericin B induced signal transduction and inflammatory cytokine release. In primary murine macrophages and human cell lines expressing TLR2, CD14, and the adapter protein MyD88, amphotericin induced NF-κB-dependent reporter activity and cytokine release, whereas cells deficient in any of these failed to respond. Cells with TLR4 mutation were less responsive to amphotericin B stimulation than cells expressing normal TLR4 [1]. Amphotericin B could interact with cholesterol, the major sterol of mammal membranes, thus limiting the usefulness of Amphotericin B due to its relatively high toxicity [2]. Low AmB concentrations (≤ 0.1 μM) induced a polarization potential in KCl-loaded liposomes suspended in an iso-osmotic sucrose solution, indicating K+ leakage. AmB (> 0.1 μM) allowed cations and anions movements. LPs suspended in an iso-osmotic NaCl solution and exposed to AmB (0.05 μM) exhibited a nearly total collapse of the negative membrane potential, indicated that Na+ entered into the cells [3].

In vivo: Amphotericin B prolonged the incubation time and decreased PrPSc accumulation in the hamster scrapie model. Amphotericin B markedly resulted in reduction of PrPSc levels in mice with transmissible subacute spongiform encephalopathies (TSSE) [4].

References:
[1]. Sau K1,Mambula SS,Latz E,Henneke P,Golenbock DT,Levitz SM.The antifungal drug amphotericin B promotes inflammatory cytokine release by a Toll-like receptor- and CD14-dependent mechanism.J Biol Chem.2003 Sep 26;278(39):37561-8. Epub 2003 Jul 14.
[2]. Barwicz J1,Tancrède P.The effect of aggregation state of amphotericin-B on its interactions with cholesterol- or ergosterol-containing phosphatidylcholine monolayers.Chem Phys Lipids.1997 Feb 28;85(2):145-55.
[3]. Ramos H1,Valdivieso E,Gamargo M,Dagger F,Cohen BE.Amphotericin B kills unicellular leishmanias by forming aqueous pores permeable to small cations and anions.J Membr Biol.1996 Jul;152(1):65-75.
[4]. Demaimay R1,Adjou K,Lasmézas C,Lazarini F,Cherifi K,Seman M,Deslys JP,Dormont D.Pharmacological studies of a new derivative of amphotericin B, MS-8209, in mouse and hamster scrapie.J Gen Virol.1994 Sep;75 ( Pt 9):2499-503.

文献引用

1. Perni S, Lavorato M, Beam KG. "De novo reconstitution reveals the proteins required for skeletal muscle voltage-induced Ca(2+) release." Proc Natl Acad Sci U S A. 2017 Dec 26;114(52):13822-13827. PMID:29229815

Chemical Properties

StorageStore at -20°C
M.Wt924.08
Cas No.1397-89-3
FormulaC47H73NO17
Solubility≥46.2mg/mL in DMSO
SDFDownload SDF
Canonical SMILESCC1C=CC=CC=CC=CC=CC=CC=CC(CC2C(C(CC(O2)(CC(CC(C(CCC(CC(CC(=O)OC(C(C1O)C)C)O)O)O)O)O)O)O)C(=O)O)OC3C(C(C(C(O3)C)O)N)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

腹膜巨噬细胞; 表达TLR2和CD14的HEK293细胞

溶解方法

在DMSO中的溶解度>46.2mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

1、2和4 μg/ml

应用

在来自CD14敲除小鼠(C57BL/6 CD14 - / - )和CD14野生型(C57BL/6 CD14 + / +)小鼠的腹膜巨噬细胞中,Amphotericin B无法诱导来自CD14 - / - 小鼠的巨噬细胞中TNF-α的产生。表达TLR2和CD14的HEK293细胞对Amphotericin B(1,2和4μg/ ml)的响应更强烈。

动物实验[2]:

动物模型

仓鼠瘙痒病模型

剂量

2.5 mg/kg; 接种后0-7天注射

应用

在瘙痒病大脑内感染的仓鼠中,Amphotericin B显著延长生存时间14.7天。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

[1]. Sau K1,Mambula SS,Latz E,Henneke P,Golenbock DT,Levitz SM.The antifungal drug amphotericin B promotes inflammatory cytokine release by a Toll-like receptor- and CD14-dependent mechanism.J Biol Chem.2003 Sep 26;278(39):37561-8. Epub 2003 Jul 14.

[2]. Demaimay R1,Adjou K,Lasmézas C,Lazarini F,Cherifi K,Seman M,Deslys JP,Dormont D.Pharmacological studies of a new derivative of amphotericin B, MS-8209, in mouse and hamster scrapie.J Gen Virol.1994 Sep;75 ( Pt 9):2499-503.

质量控制

化学结构

Amphotericin B

相关生物数据

Amphotericin B