Benznidazole

製品コードS3741 バッチS374101

印刷

化学情報

Chemical Structure Synonyms Radanil Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C12H12N4O3
分子量 260.25 CAS No. 22994-85-0
Solubility (25°C)* 体外 DMSO 52 mg/mL (199.8 mM)
Ethanol 5 mg/mL (19.21 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Benznidazole (Radanil) is a nitroimidazole derivative having an antiprotozoal activity by interfering with parasite protein biosynthesis, influencing cytokines production and stimulating host phagocytosis.
in vitro Benznidazole (BZL) 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 BZL is a reversible process, not accompanied by significant cell death. Besides its trypanocidal activity, BZL also has an immunomodulatory effect on macrophages by blocking the transcription of some pro-inflammatory mediators without altering interleukin 10 expression[1].
in vivo In mice, oral administration of Benznidazole (100 mg/kg): the time to reach maximum concentration (Tmax) in plasma was 0.83 h, and the maximum concentration (Cmax) in plasma was 41.61 μg/ml. The elimination half-life (t1/2b) 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. 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. 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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 THP-1 cells
濃度 0.1, 0.5 or 1 mM
反応時間 24 or 48 h
実験の流れ

20000 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 ℃, the MTT solution was removed and precipitated formazan was solubilized in 200 mL DMSO. Formazan production was then measured at OD545nm in a micro plate spectrophotometer, with DMSO as blank.
動物実験 動物モデル Swiss mice 
投薬量 100 mg/kg
投与方法 by gavage

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Activity of Drug Combinations against Mycobacterium abscessus Grown in Aerobic and Hypoxic Conditions [ Microorganisms, 2022, 10(7)1421] PubMed: 35889140

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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