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Amphotericin B Sale

(Synonyms: 两性霉素B) 目录号 : GC14092

An antifungal macrolide

Amphotericin B Chemical Structure

Cas No.:1397-89-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥385.00
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100mg
¥350.00
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500mg
¥686.00
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1g
¥1,120.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

peritoneal macrophages; HEK293 cells expressing TLR2 and CD14

Preparation method

The solubility of this compound in DMSO is >46.2mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1, 2, and 4 μg/ml

Applications

In peritoneal macrophages from CD14 knockout mice (C57BL/6 CD14–/–) and CD14 wild-type (C57BL/6 CD14+/+) mice, Amphotericin B failed to induce the production of TNF-α in macrophages from CD14–/– mice. HEK293 cells expressing TLR2 and CD14 responded more strongly to Amphotericin B (1, 2, and 4 μg/ml).

Animal experiment [2]:

Animal models

hamster scrapie model

Dosage form

2.5 mg/kg; p.i. injection from 0 to 7 days

Application

In hamsters infected intracerebrally with scrapie, Amphotericin B significantly prolonged the survival time by 14.7 days.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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.

产品描述

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].

两性霉素B是一种多烯类抗真菌抗生素,由结节链霉菌菌株产生,其IC50为0.028–0.290μg/ml。

体外:两性霉素B是治疗许多危及生命的真菌感染最有效的药物。在表达TLR2和CD14的细胞中,两性霉素B诱导信号转导和炎性细胞因子释放。在表达TLR2、CD14和衔接蛋白MyD88的原代鼠巨噬细胞和人细胞系中,两性霉素诱导NF-κB依赖性报告基因活性和细胞因子释放,而缺乏任何这些的细胞都没有反应。与表达正常TLR4的细胞相比,具有TLR4突变的细胞对两性霉素B刺激的反应较弱[1]。两性霉素B可能与哺乳动物膜的主要固醇胆固醇相互作用,因此由于其相对较高的毒性而限制了两性霉素的用途[2]。

低AmB浓度(≤0.1μM)在悬浮于等渗蔗糖溶液中的KCl负载脂质体中诱导极化电位,表明K+渗漏。AmB(>0.1μM)允许阳离子和阴离子运动。悬浮在等渗NaCl溶液中并暴露于AmB(0.05μM)的LPs表现出负膜电位几乎完全崩溃,表明Na+进入细胞[3]。

体内:两性霉素B延长了仓鼠瘙痒模型中的孵育时间并减少了PrPSc的积累。两性霉素B可显著降低传播性亚急性海绵状脑病(TSSE)小鼠的PrPSc水平[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.

Chemical Properties

Cas No. 1397-89-3 SDF
别名 两性霉素B
Canonical SMILES CC1C=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
分子式 C47H73NO17 分子量 924.08
溶解度 ≥ 46.2mg/mL in DMSO 储存条件 4°C, protect from light
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 1.0822 mL 5.4108 mL 10.8216 mL
5 mM 0.2164 mL 1.0822 mL 2.1643 mL
10 mM 0.1082 mL 0.5411 mL 1.0822 mL
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