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/ Amphotericin B/两性霉素B

Amphotericin B/两性霉素B {[allProObj[0].p_purity_real_show]}

货号：A119196 同义名： 两性霉素B / LNS-AmB; NSC 527017

Amphotericin B是一种多烯类抗真菌药，源自链霉菌，通过特异性结合真菌细胞膜甾醇成分（如麦角固醇）改变膜通透性，促使胞内钾离子及氨基酸外泄，最终导致真菌代谢紊乱和死亡。因细菌细胞膜缺乏甾醇而对细菌无抑制作用，Amphotericin B可与双抗一起使用，预防细胞受真菌和细菌污染。

Amphotericin B/两性霉素B 化学结构 CAS号：1397-89-3
Amphotericin B/两性霉素B 化学结构
CAS号：1397-89-3
Amphotericin B/两性霉素B 3D分子结构
CAS号：1397-89-3
Amphotericin B/两性霉素B 化学结构 CAS号：1397-89-3
Amphotericin B/两性霉素B 3D分子结构 CAS号：1397-89-3
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Amphotericin B/两性霉素B 纯度/质量文件 产品仅供科研

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Amphotericin B/两性霉素B 生物活性

描述 Amphotericin B (AmB) is the most effective drug for treating many life-threatening fungal infections. TLR2 (Toll-like receptors) and CD14 are required for amphotericin B-dependent inflammatory stimulation of innate immune cells and that TLR4 may also provide stimulation of these cells[1]. AmB only kills unicellular Leishmania promastigotes (LPs) when aqueous pores permeable to small cations and anions are formed. At low concentrations (≤0.1 microM), AmB was found to be nonlethal against LPs but, above this concentration, leishmanias were rapidly killed[3]. Amphotericin B treatment of hamsters infected with scrapie strain 263K prolongs the incubation period of the disease [4].
体内研究 To test antifungal activity in vivo, Amphotericin B (0.25-4 mg/kg) was administered as a single intraperitoneal injection to C. albicans K-1-infected ICR/Swiss mice. Only the highest single dose of Amphotericin B treatment significantly reduced the number of colonies compared to the number of colonies at the start of treatment [7].
体外研究 Human normal colonic epithelial cells CCD 841 CoTr and human colorectal cancer cells HT-29 were treated with Amphotericin B (0.05-25 µg/mL) for 24 h. Cell viability was measured by Neutral Red method. Higher concentrations of Amphotericin B were toxic to CCD 841 CoTr and HT-29 cells with IC50 values of 8.7 µg/mL and 21.2 µg/mL, respectively[5]. Candida albicans were treated with Amphotericin B (100 µM) for 4-16 min and imaged using the FLIM technique.Amphotericin B preferentially binds to the cell wall and does not efficiently cross the barrier covering the cell membrane.Amphotericin B is able to pass through the cell wall barrier of young cells more readily in the emergence phase. Amphotericin B can more easily pass through the cell wall barrier of young cells at the emergence stage [6].

Amphotericin B/两性霉素B 细胞实验

Cell Line
Concentration Treated Time Description References
Mouse Embryonic Fibroblasts (MEFs) 25 ng/ml Used for culturing MEFs to study the effect of GPC1 on cell migration Oncogene. 2012 May 17;31(20):2535-44.
Human and mice immune cells 250 ng/mL Used for the culture of immune cells to maintain a sterile environment. Cell Death Dis. 2019 Feb 8;10(2):113.
Human and mice stromal cells 250 ng/mL Used for the culture of stromal cells to maintain a sterile environment. Cell Death Dis. 2019 Feb 8;10(2):113.
bone marrow-derived macrophages (BMM) 5 μg/ml 3 weeks Used to inhibit fungal growth to assess the growth of Mycobacterium tuberculosis. mBio. 2022 Oct 26;13(5):e0108622.
L. major promastigotes 207 nM 44 h Determine the growth inhibitory activity of Amphotericin B against L. major promastigotes, EC50 was 207 nM PLoS Negl Trop Dis. 2009 Nov 3;3(11):e540.
L. major axenic amastigote-like parasites 380 nM 144 h Determine the growth inhibitory activity of Amphotericin B against L. major axenic amastigote-like parasites, EC50 was 380 nM PLoS Negl Trop Dis. 2009 Nov 3;3(11):e540.

Amphotericin B/两性霉素B 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Wild-type mice Oral 0.2 mL of 0.1 mg/ml Every 12 hours for three days To deplete the gut microbiota in mice for studying its impact on pancreatic tumors Cancer Res. 2020 Mar 1;80(5):1088-1101
Mice Chronic Social Defeat Stress model Intraperitoneal injection 1 mg/kg Single injection Amphotericin B liposomes reversed and prevented behavioral abnormalities in mice induced by chronic social defeat stress (CSDS) by activating the innate immune system. Front Pharmacol. 2022 Jul 15;13:918177
Mice Antibiotic-induced gut microbiota depletion model Gavage 1 mg/kg Every 12 hours for three days To study the effect of Amphotericin B on sleep promotion in mice through antibiotic-induced gut microbiota depletion. The results showed that antibiotic treatment blocked Amphotericin B-induced alterations in sleep behavior and increases in 5-HT levels. Sci Rep. 2021 Jul 1;11(1):13660
Mice Pasteurella multocida type‐A (PmCQ2) infection model Drinking water 0.1 mg/mL Continued for 3 weeks To investigate the impact of intestinal mycobiota dysbiosis on lung inflammation, the results showed that Amphotericin B treatment increased mortality and lung bacterial loads, and enhanced the production of inflammatory cytokines in the serum and lung. Imeta. 2024 Sep 14;3(5):e241
Balb/c mice L. major infection model Subcutaneous injection 12.5 mg/kg Once daily for 21 days Evaluate the efficacy of Amphotericin B in the L. major infected mouse model, results showed Amphotericin B effectively reduced footpad swelling PLoS Negl Trop Dis. 2009 Nov 3;3(11):e540.
Mice C57BL/6J mice Oral 0.2 g/L Water changes every 3 days for 2 weeks Used for antibiotic pre-treatment to eliminate the regulatory activity of the IH microbiota Cell Host Microbe. 2022 Sep 14;30(9):1295-1310.e8

Amphotericin B/两性霉素B 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00163111 Candidiasis Phase 3 Completed - -
NCT00370825 Visceral Leishmaniasis Phase 2 Completed - India ... 展开 >> Kala-azar Medical Research Center Muzaffarpur, Bihar, India, 842001 收起 <<
NCT00002742 Chronic Myeloproliferative Dis... 展开 >>orders Infection Leukemia Lymphoma Multiple Myeloma and Plasma Cell Neoplasm Myelodysplastic Syndromes 收起 << Phase 3 Completed - -

Amphotericin B/两性霉素B 参考文献

[1]Sau K, 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;278(39):37561‐37568

[2]Barwicz J, Tancrede 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 H, 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;152(1):65‐75

[4]Demaimay R, Adjou K, Lasmézas C, et al. Pharmacological studies of a new derivative of amphotericin B, MS-8209, in mouse and hamster scrapie. J Gen Virol. 1994;75 ( Pt 9):2499‐2503

[5]Grela E, et al. Imaging of human cells exposed to an antifungal antibiotic amphotericin B reveals the mechanisms associated with the drug toxicity and cell defence. Sci Rep. 2018 Sep 14;8(1):14067.

[6]Grela E, et al. Modes of the antibiotic activity of amphotericin B against Candida albicans. Sci Rep. 2019 Nov 19;9(1):17029.

[7]Andes D, Pet al. Pharmacodynamics of amphotericin B in a neutropenic-mouse disseminated-candidiasis model. Antimicrob Agents Chemother. 2001 Mar;45(3):922-6.

Amphotericin B/两性霉素B 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.08mL

0.22mL

0.11mL

5.41mL

1.08mL

0.54mL

10.82mL

2.16mL

1.08mL

Amphotericin B/两性霉素B 技术信息

CAS号1397-89-3
分子式C47H73NO17
分子量 924.08
SMILES Code C[C@H]([C@@H](O)[C@@H](C)[C@H](C)OC1=O)/C=C/C=C/C=C/C=C/C=C/C=C/C=C/[C@H](O[C@]2([H])O[C@H](C)[C@@H](O)[C@H](N)[C@@H]2O)C[C@@]3([H])[C@H](C(O)=O)[C@@H](O)C[C@](C[C@@H](O)C[C@@H](O)[C@H](O)CC[C@@H](O)C[C@@H](O)C1)(O)O3
MDL No. MFCD00877763
别名 两性霉素B ;LNS-AmB; NSC 527017; Fungizone
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C
溶解方案

DMSO: 50 mg/mL(54.11 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二

Tags: Amphotericin B | LNS-AmB;NSC 527017;Fungizone | 两性霉素B | Drug Standard | Anti-fungal Antibiotic | Insect Repellent | Macrolide | Antifungal | AmBeed-信号通路专用抑制剂 | Amphotericin B/两性霉素B 纯度/质量文件 | Amphotericin B/两性霉素B 生物活性 | Amphotericin B/两性霉素B 临床数据 | Amphotericin B/两性霉素B 参考文献 | Amphotericin B/两性霉素B 实验方案 | Amphotericin B/两性霉素B 技术信息

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