Benserazide  (Synonyms: Ro 4-4602)

Benserazide is an aromatic L-amino acid decarboxylase (AADC) and L-DOPA decarboxylase inhibitor. Benserazide is also a PKM2 inhibitor. Benserazide directly binds to and blocks PKM2 enzyme activity, leading to inhibition of aerobic glycolysis concurrent up-regulation of OXPHOS. Benserazide can be used for the study of Parkinson's disease and melanoma^[1][2][3].

Benserazide and Levodopa (LD) individually and in combination (Benserazide + LD) (25 μM; 0 hour, 12 hours, 24 hours and 168 hours; SH-SY5Y) treatment inhibit protein aggregation and have the ability to minimise the amyloid-induced cytotoxicity in human neuroblastoma cell line. Benserazide and LD both can act as efficient inhibitors of the formation of cytotoxic HSA aggregates, and the inhibitory effects are more pronounced when both of these drugs are added simultaneously^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Benserazide (5-50 mg/kg; intraperitoneal injection; male Wistar rats) treatment of 6-OHDA-lesioned rats increases exogenous L-DOPA-derived extracellular DA levels, the time to reach the peak DA levels are significantly prolong by Benserazide dose-dependently. The AADC activity in the denervates striatal tissues shows a significant decrease by 10 mg/kg and 50 mg/kg Benserazide. Benserazide reduces the central AADC activity in the striatum of rats with nigrostriatal denervation, which leads to changes in the metabolism of exogenous L-DOPA^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

257.24

C₁₀H₁₅N₃O₅

322-35-0

NC(C(NNCC1=CC=C(C(O)=C1O)O)=O)CO

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Zhou Y, et al. Benserazide is a novel inhibitor targeting PKM2 for melanoma treatment. Int J Cancer. 2020 Jul 1;147(1):139-151.  [Content Brief]

  [2]. Shen H, et al. Effects of benserazide on L-DOPA-derived extracellular dopamine levels and aromatic L-amino acid decarboxylase activity in the striatum of 6-hydroxydopamine-lesioned rats. Tohoku J Exp Med. 2003 Mar;199(3):149-59.  [Content Brief]

  [3]. Chandel TI, et al. A multiparametric analysis of the synergistic impact of anti-Parkinson's drugs on the fibrillation of human serum albumin. Biochim Biophys Acta Proteins Proteom. 2019 Mar;1867(3):275-285.  [Content Brief]