| Size | Price | Stock | Qty |
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| 2g |
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| 5g |
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| 10g |
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| 25g |
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| Other Sizes |
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Benserazide HCl (Ro-44602; Serazide; Ro 4-4602), the hydrochloride salt of Benserazide, is a carbohydrazide-based, peripherally acting inhibitor of aromatic L-amino acid decarboxylase/AADC or DOPA decarboxylase and a medication used in combination with levodopa (madopar) to treat Parkinson's disease, parkinsonism, and restless leg syndrome.
| ln Vitro |
Treatment with benserazide hydrochloride (BH) and levodopa (LD) alone or in combination (benserazide hydrochloride + LD) (25 μM; 0 hours, 12 hours, 24 hours, and 168 hours; SH-SY5Y) decreases protein aggregation and can limit protein aggregation. Amyloid-induced cytotoxicity in human neuroblastoma cell lines. Both benserazide hydrochloride and LD can be efficient inhibitors of the formation of cytotoxic HSA aggregates, and the inhibitory effect is more visible when the two medicines are introduced at the same time [2].
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| ln Vivo |
Benserazide (5–50 mg/kg; intraperitoneal injection; male Wistar rats) treatment raised exogenous L-DOPA-derived extracellular DA levels and considerably extended the time to peak DA levels in 6-OHDA-injured rats. ..Depend on. With 10 mg/kg and 50 mg/kg benserazide, there was a substantial decrease in AADC activity in denervated striatal tissue. Benserazide alters the metabolism of exogenous L-DOPA by lowering central AADC activity in the striatum of rats suffering from nigrostriatal denervation [1].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: SH-SY5Y Cell Tested Concentrations: 25 μM Incubation Duration: 0 hrs (hours), 12 hrs (hours), 24 hrs (hours) and 168 hrs (hours) Experimental Results: Enhanced cell viability and inhibited cytotoxic human serum albumin (HSA) aggregates Formation. |
| Animal Protocol |
Animal/Disease Models: Male Wistar rat 6-hydroxydopamine (6-OHDA) (8 Ag/4 Al)[1]
Doses: 5 mg/kg, 10 mg/kg or 50 mg/kg (pharmacokinetic/PK/PK study) Give Medication: intraperitoneal (ip) injection. Experimental Results: Extracellular DA levels derived from exogenous L-DOPA increased, and the time to reach peak DA levels was Dramatically prolonged in a dose-dependent manner. AADC activity in denervated striatal tissue was Dramatically diminished at 10 mg/kg and 50 mg/kg. |
| References |
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| Additional Infomation |
Benserazide hydrochloride is a hydrochloride that is the monohydrochloride salt of benserazide. An aromatic-L-amino-acid decarboxylase inhibitor (DOPA decarboxylase inhibitor) that does not enter the central nervous system, it is used as an adjunct to levodopa in the treatment of parkinsonism. By preventing the conversion of levodopa to dopamine in the periphery, it causes an increase in the amount of levodopa reaching the central nervous system and so reduces the required dose. Benserazide hydrochloride has no antiparkinson actions when given alone. It has a role as an antiparkinson drug, an EC 4.1.1.28 (aromatic-L-amino-acid decarboxylase) inhibitor and a dopaminergic agent. It contains a benserazide(1+).
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| Molecular Formula |
C10H16CLN3O5
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|---|---|
| Molecular Weight |
293.7041
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| Exact Mass |
293.077
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| CAS # |
14919-77-8
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| Related CAS # |
Benserazide;322-35-0;Benserazide-d3 hydrochloride
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| PubChem CID |
26964
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| Appearance |
White to off-white solid powder
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| Boiling Point |
574.2ºC at 760 mmHg
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| Melting Point |
146°C
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| LogP |
0.527
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
19
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| Complexity |
278
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ULFCBIUXQQYDEI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H15N3O5.ClH/c11-6(4-14)10(18)13-12-3-5-1-2-7(15)9(17)8(5)16;/h1-2,6,12,14-17H,3-4,11H2,(H,13,18);1H
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| Chemical Name |
2-amino-3-hydroxy-N'-[(2,3,4-trihydroxyphenyl)methyl]propanehydrazide;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~340.48 mM)
H2O : ≥ 50 mg/mL (~170.24 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.08 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (340.48 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4048 mL | 17.0242 mL | 34.0483 mL | |
| 5 mM | 0.6810 mL | 3.4048 mL | 6.8097 mL | |
| 10 mM | 0.3405 mL | 1.7024 mL | 3.4048 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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