| CAS |
22994-85-0 |
| Chinese Name |
苄哒唑 |
| English Name |
Benznidazole |
| Synonyms |
苄硝唑 |
| Molecular Formula |
C12H12N4O3 |
| Molecular Weight |
260.25 |
| Solubility |
Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
| Purity |
≥98% |
| Appearance |
Off-white to yellow Solid |
| Storage |
Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD00243089 |
| SMILES |
O=C(NCC1=CC=CC=C1)CN2C=CN=C2[N+]([O-])=O |
| InChIKey |
CULUWZNBISUWAS-UHFFFAOYSA-N |
| InChI |
InChI=1S/C12H12N4O3/c17-11(14-8-10-4-2-1-3-5-10)9-15-7-6-13-12(15)16(18)19/h1-7H,8-9H2,(H,14,17) |
| PubChem CID |
31593 |
| Target Point |
Parasite |
| Passage |
Anti-infection |
| Background |
It is a nitroimidazole derivative, which can interfere with the biosynthesis of parasite proteins, affect the production of cytokines, stimulate the phagocytosis of the host, and has antiprotozoal activity. |
| Biological Activity |
Benznidazole (Radanil)是一种硝基咪唑衍生物，能够干扰寄生虫蛋白质的生物合成、影响其细胞因子的产生、刺激宿主的吞噬作用，因而具有抗原虫活性。[1-2] |
| 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]. |
| Cell Experiment |
Animal Models: Swiss mice ; Dosages: 100 mg/kg; Administration: by gavage[2] |
| Animal Experiment |
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.[1] |
| Data Literature Source |
[1] Calvo KL，et al. Immunopharmacol Immunotoxicol. 2013，35(4):478-86.
[2] Perin L，et al. Antimicrob Agents Chemother. 2017，61(4). pii: e |
| Unit |
Bottle |
| Specification |
25mg 50mg |
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