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Amphotericin B

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Chemical Structure| 1397-89-3 同义名 : 两性霉素B ;LNS-AmB;NSC 527017;Fungizone
CAS号 : 1397-89-3
货号 : A119196
分子式 : C47H73NO17
纯度 : ≥750ug/mg
分子量 : 924.079
MDL号 : MFCD00877763
存储条件:

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

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

动物实验配方:

IP 2% DMSO+2% Tween80+30% PEG300+water 1 mg/mL clear

PO 0.5% CMC-Na 36 mg/mL suspension

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].
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 - -
实验方案
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

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