Amphotericin-B - Fungal 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAmphotericin BCat. No.: HY-B0221CAS No.: 1397-89-3分式: CHNO分量: 924.08作靶点: Fungal作通路: Anti-infection储存式: 4C, protect from light, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight, stored under ni

2、trogen)溶解性数据体外实验 DMSO : 100 mg/mL (108.22 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 10 mg/mL (10.82 mM); Suspended solution; Need ultrasonic and warming2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 10 mg/mL (10.82 mM); Suspended solution; Need ultrasonic and warming1/3 Mas

3、ter of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Amphotericin B针对多种真 病原体的多烯抗真 (fungal) 剂。 它与麦甾醇不可逆地结合，导致膜完整性破坏并最终导致细胞死亡。IC50 & Target Fungal 1体外研究 Amphotericin B administration is limited by infusion-related toxicity, including fever and chills, an effectpostulated to result from pro

4、inflammatory cytokine production by innate immune cells. Amphotericin Binduces signal transduction and inflammatory cytokine release from cells expressing TLR2 and CD14 1.Amphotericin B interacts with cholesterol, the major sterol of mammal membranes, thus limiting theusefulness of Amphotericin B du

5、e to its relatively high toxicity. Amphotericin B is dispersed as a pre-micellaror as a highly aggregated state in the subphase 2. Amphotericin B only kills unicellular Leishmaniapromastigotes (LPs) when aqueous pores permeable to small cations and anions are formed. Amphotericin B(0.1 mM) induces a

6、 polarization potential, indicating K+ leakage in KCl-loaded liposomes suspended in aniso-osmotic sucrose solution. Amphotericin B (0.05 mM) exhibits a nearly total collapse of the negativemembrane potential, indicating Na+ entry into the cells 3.体内研究 Amphotericin B results in prolonging the incubat

7、ion time and decreasing PrPSc accumulation in the hamsterscrapie model. Amphotericin B markedly reduces PrPSc levels in mice with transmissible subacutespongiform encephalopathies (TSSE) 4. Amphotericin B exerts a direct effect on Plasmodium falciparumand influences eryptosis of infected erythrocyte

8、s, parasitemia and hostsurvival in murine malaria.Amphotericin B tends to delay the increase of parasitemia and significantly delays host death plasmodiumberghei-infected mice 5.PROTOCOLKinase Assay 1 THP-1 and HEK293 cells are transiently transfected using DEAE-dextran and Polyfect reagent, respect

9、ively.Plasmids transfected contain genes coding for the NF-B-dependent pELAM-luc luciferase reporter, TLR2,TLR4, CD14, and MD2. Cells (5105 THP-1 or 1105 HEK293) are added to 12-well plates, washed after 18h, and stimulated for 5 h. Cells are then lysed with reporter lysis buffer as directed, and ly

10、sates are analyzedfor luminescence using Promega luciferase substrate and a Monolight 3010 luminometer.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 3 The kinetics of cell death induced by AmB against Leishmania promastigotes is followed by

11、 using fluorometrywith the DNA-binding compound ethidium bromide (EB). Fluorescence measurements are performed on aSPEX Fluorolog II spectrophotometer at 365-580 nm excitation-emission wavelengths. Promastigotes at afinal concentration of 25106 cells/mL are incubated for 5 min with gentle stirring i

12、n the fluorescence cuvettewith 2 mL of different buffered solutions but always containing 10 mM glucose and EB (50 mM). After signalstabilization is achieved, AmB is added and dissolved in dimethylsulfoxide. Maximal EB incorporation isalways obtained by adding digitonin (50 mg/mL). All solutions use

13、d are buffered with 75 mM TRIS (pH 4 7.6)and contain 150 mM NaCl (BNa+), 150 mM KCl (BK+), 150 mM choline chloride, and 100 mM sucrose, 100mM NaCl. The osmolarity of all solutions is always adjusted to 3905 mOsm using an advanced instrumentSW2 osmometer.2/3 Master of Small Molecules 您边的抑制剂师www.MedCh

14、emEMCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Neuropharmacology. 2019 Apr 4;151:33-44. Am J Physiol Cell Physiol. 2019 Aug 1;317(2):C277-C286. Evid Based Complement Alternat Med. 2015;2015:639412.See more customer validations on HYPERLI

15、NK / www.MedChemEREFERENCES1. Sau K, et al. The antifungal drug amphotericin B promotes inflammatory cytokine release by a Toll-like receptor- and CD14-dependentmechanism. J Biol Chem. 2003 Sep 26;278(39):37561-8. Epub 2003 Jul 14.2. Barwicz J, et al. The effect of aggregation state of amphotericin-

16、B on its interactions with cholesterol- or ergosterol-containingphosphatidylcholine monolayers. Chem Phys Lipids. 1997 Feb 28;85(2):145-55.3. Ramos H, et al. Amphotericin B kills unicellular leishmanias by forming aqueous pores permeable to small cations and anions. J MembrBiol. 1996 Jul;152(1):65-7

17、5.4. Demaimay R, et al. Pharmacological studies of a new derivative of amphotericin B, MS-8209, in mouse and hamster scrapie. J GenVirol. 1994 Sep;75 (Pt 9):2499-503.5. Adams ML, et al. Amphotericin B encapsulated in micelles based on poly(ethylene oxide)-block-poly(L-amino acid) derivatives exertsreduced in vitro hemolysis but maintains potent in vivo antif