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  3. Benserazide hydrochloride

Benserazide hydrochloride  (Synonyms: Ro 4-4602 hydrochloride)

Cat. No.: HY-B0404A Purity: 99.68%
Handling Instructions Technical Support

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

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Benserazide hydrochloride

Benserazide hydrochloride 화학구조

CAS No. : 14919-77-8

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
500 mg 해외재고보유
1 g 해외재고보유
5 g 해외재고보유
10 g   견적 받기  
50 g   견적 받기  

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 7 publication(s) in Google Scholar

Other Forms of Benserazide hydrochloride:

Top Publications Citing Use of Products
  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

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

In Vitro

Benserazide hydrochloride (BH) and Levodopa (LD) individually and in combination (Benserazide hydrochloride + 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 hydrochloride 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.

Cell Viability Assay[2]

Cell Line: SH-SY5Y cells
Concentration: 25 μM
Incubation Time: 0 hour, 12 hours, 24 hours and 168 hours
Result: Enhanced cell viability, and inhibited the formation of cytotoxic human serum albumin (HSA) aggregates.
In Vivo

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.

Animal Model: Male Wistar rats with 6-hydroxydopamine (6-OHDA) (8 Ag/4 Al)[1]
Dosage: 5 mg/kg, 10 mg/kg or 50 mg/kg (Pharmacokinetic study)
Administration: Intraperitoneal injection
Result: Increased in exogenous L-DOPA-derived extracellular DA levels, the time to reach the peak DA levels were significantly prolonged in a dose-dependent fashion. The AADC activity in the denervated striatal tissues showed a significant decreased by 10 mg/kg and 50 mg/kg.
분자량

293.70

화학식

C10H16ClN3O5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

선적

Room temperature in continental US; may vary elsewhere.

보관

4°C, sealed storage, away from moisture

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

용액&용해도
In Vitro: 

DMSO : 100 mg/mL (340.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 50 mg/mL (170.24 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 몰농도 계산기

  • 농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (7.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (7.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (340.48 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
순도&문서

Purity: 99.68%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.4048 mL 17.0242 mL 34.0483 mL 85.1209 mL
5 mM 0.6810 mL 3.4048 mL 6.8097 mL 17.0242 mL
10 mM 0.3405 mL 1.7024 mL 3.4048 mL 8.5121 mL
15 mM 0.2270 mL 1.1349 mL 2.2699 mL 5.6747 mL
20 mM 0.1702 mL 0.8512 mL 1.7024 mL 4.2560 mL
25 mM 0.1362 mL 0.6810 mL 1.3619 mL 3.4048 mL
30 mM 0.1135 mL 0.5675 mL 1.1349 mL 2.8374 mL
40 mM 0.0851 mL 0.4256 mL 0.8512 mL 2.1280 mL
50 mM 0.0681 mL 0.3405 mL 0.6810 mL 1.7024 mL
60 mM 0.0567 mL 0.2837 mL 0.5675 mL 1.4187 mL
80 mM 0.0426 mL 0.2128 mL 0.4256 mL 1.0640 mL
100 mM 0.0340 mL 0.1702 mL 0.3405 mL 0.8512 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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상품명:
Benserazide hydrochloride
Cat. No.:
HY-B0404A
수량:
MCE Japan Authorized Agent: