苄硝唑 T4982

Product Introduction
Bioactivity


英文名: Benznidazol

描述: Benznidazol (Benznidazole) 是一种抗寄生虫药物，对哥伦比亚 T. cruzi 菌株的 IC50值为 20.35 μM，有潜力研究美洲锥虫病。

细胞实验: 20000 THP-1 cells in 200 mL of complete medium were incubated in quadruplicate in a 96-well plate in the presence of BZL (0.1, 0.5 and 1 mM) or vehicle (0.1% DMSO) for 24 or 48 h and then 20 mL of MTT solution (5 mg/mL in phosphate-buffered saline [PBS]) was added to each well. After 2 h at 37 °C, the MTT solution was removed and precipitated formazan was solubilized in 200 mL DMSO. Formazan production was then measured at OD545nm in a microplate spectrophotometer, with DMSO as blank.

体外活性: Benznidazole inhibits the proliferation of leukemic non-adherent cells by controlling cell cycle at G0/G1 cell phase through up-regulation of p27. Growth inhibition induced by Benznidazole is a reversible process, not accompanied by significant cell death. Benznidazole also has an immunomodulatory effect on macrophages by blocking the transcription of some pro-inflammatory mediators without altering interleukin 10 expression [1].

体内活性: In Wistar rats treated orally, Tmaxs of Benznidazole are 2.0 and 1.1 h, respectively. Tmaxs of 15, 30, or 60 min, depending on the dose, in BALB/c mice following intraperitoneal treatment and Tmaxs of 1 to 5 h for dogs treated orally. In mice, Benznidazole (100 mg/kg, p.o.): Tmax in plasma, 0.83 h; Cmax in plasma: 41.61 μg/ml. The elimination half-life (t1/2) of Benznidazole was 2.03 h, and mean residence time (MRT) was 3.86 h. The volume of distribution (V) and clearance (CL), both as a function of Benznidazole bioavailability (F), were 38.81 ml and 13.29 ml/h, respectively. Benznidazole can cross the blood-brain barrier and exert its action in cases of central nervous system parasitism. However, other studies have indicated that BNZ has toxic effects in the central nervous system. Dogs orally treated with BNZ presented encephalopathy with multifocal characteristics and clinical, pathological, and neurological disorders that were dose-dependent and time-dependent. Benznidazole biodistribution occurs broadly, reaching the heart and colon, which are the most relevant organs for T. cruzi infection, and also the spleen, brain, liver, lungs, and kidneys [2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Methanol : 50 mg/mL
DMSO : 60 mg/mL (230.55 mM)


关键字: Ro71051 | inhibit | Inhibitor | Parasite | Ro-71051 | Benznidazol

相关产品: Aurein 3.2 | Pentamidine isethionate | Olsalazine disodium | Albendazole | Sulbactam | Nitrofurazone | Clinafloxacin | Sulfabenzamide | SulfadiMethoxine sodium | Tobramycin

相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | Approved Drug Library | ReFRAME Related Library | Drug-induced Liver Injury (DILI) Compound Library | Drug-Fragment Library | Bioactive Compounds Library Max | Human Metabolite Library | Anti-Parasitic Compound Library | Anti-Infection Compound Library

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