1. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  2. Reactive Oxygen Species (ROS)
  3. 5-Aminolevulinic acid hydrochloride

5-Aminolevulinic acid hydrochloride  (Synonyms: 5-ALA hydrochloride; δ-Aminolevulinic acid hydrochloride; 5-Amino-4-oxopentanoic acid hydrochloride)

Cat. No.: HY-N0305 Purity: 99.61%
Handling Instructions Technical Support

5-Aminolevulinic acid (5-ALA; δ-Aminolevulinic acid; 5-Amino-4-oxopentanoic acid) hydrochloride is an orally active heme precursor. 5-Aminolevulinic acid hydrochloride promotes aerobic energy metabolism and increases ATP levels by enhancing the activity of cytochrome c oxidase. 5-Aminolevulinic acid hydrochloride enhances LPS-induced proinflammatory cytokine production and gene activation, and restores the phagocytic activity and ROS generation capacity of neutrophils. 5-Aminolevulinic acid hydrochloride selectively accumulates protoporphyrin IX in tumor cells; as a photosensitizer and radiosensitizer, it induces ROS burst upon light or X-ray irradiation to inhibit tumor growth. 5-Aminolevulinic acid hydrochloride can be applied to the research of septic shock, melanoma, and cancer radiotherapy.

For research use only. We do not sell to patients.

CAS No. : 5451-09-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
100 mg In-stock
1 g In-stock
5 g In-stock
10 g In-stock
50 g   Get quote  

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Customer Review

Based on 20 publication(s) in Google Scholar

Top Publications Citing Use of Products

    5-Aminolevulinic acid hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2019 Jan 20;6(5):1802057.  [Abstract]

    Fluorescence intensity of PpIX produced by various CAH complexes at varying molar ratios of amine to carboxyl in B16 and A375 melanoma cells, was measured in comparison with that of free 5-ALA (8 μg/mL; 12 h).

    5-Aminolevulinic acid hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2019 Jan 20;6(5):1802057.  [Abstract]

    Inhibitory effects of light does and illumination time on cell viability of B16 cells and A375 cells treated with 5-ALA (8 µg/mL; 48 h) or CAH were evaluated by MTT assay.

    5-Aminolevulinic acid hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2019 Jan 20;6(5):1802057.  [Abstract]

    CAH specifically induced melanoma cells apoptosis in correlation with elevated intracellular ROS levels. Melanoma cell lines B16 cells and A375 cells were treated with 5-ALA (8 μg/mL; 12 h) or CAH under their optimal PDT conditions. Afterward, the cells were incubated with Annexin V-FITC (green)/PI (red), followed by FACS analysis.

    5-Aminolevulinic acid hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2019 Jan 20;6(5):1802057.  [Abstract]

    Cellular ROS levels (green) of B16 cells and A375 cells (treated with 5-ALA (8 μg/mL; 12 h) or CAH) were monitored using DCFH-DA assay with a fluorescent microscope.

    5-Aminolevulinic acid hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2019 Jan 20;6(5):1802057.  [Abstract]

    Trans-epidermal water loss (TEWL) was measured from the mice skin before and 12 h after topically applied with blank cream, 20% w/w 5-ALA cream, 20% CDG2/HA cream and 20% CAH cream with 5 min of light irradiation.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    5-Aminolevulinic acid (5-ALA; δ-Aminolevulinic acid; 5-Amino-4-oxopentanoic acid) hydrochloride is an orally active heme precursor. 5-Aminolevulinic acid hydrochloride promotes aerobic energy metabolism and increases ATP levels by enhancing the activity of cytochrome c oxidase. 5-Aminolevulinic acid hydrochloride enhances LPS-induced proinflammatory cytokine production and gene activation, and restores the phagocytic activity and ROS generation capacity of neutrophils. 5-Aminolevulinic acid hydrochloride selectively accumulates protoporphyrin IX in tumor cells; as a photosensitizer and radiosensitizer, it induces ROS burst upon light or X-ray irradiation to inhibit tumor growth. 5-Aminolevulinic acid hydrochloride can be applied to the research of septic shock, melanoma, and cancer radiotherapy[1][2][3].

    IC50 & Target

    Human Endogenous Metabolite

     

    In Vitro

    5-Aminolevulinic acid (hydrochloride) (100 μM; 24 h pre-treatment) significantly enhances LPS-induced expression of pro-inflammatory cytokine (Il1b, Il6, Tnfa) and mitochondrial (mt-Nd1, Pgc1a) genes in GM-CSF-differentiated bone marrow-derived cells from C57BL/6 mice[2].
    5-Aminolevulinic acid (hydrochloride) (0.1-100 μg/mL; 2-24 h) induces time- and concentration-dependent accumulation of porphyrins (predominantly PpIX) in B16-BL6 mouse melanoma cells in vitro[3].
    5-Aminolevulinic acid (hydrochloride) (1-100 μg/mL; 24 h prior to X-ray irradiation) enhances X-ray-induced intracellular reactive oxygen species generation in B16-BL6 mouse melanoma cells in vitro in a concentration-dependent manner, with significant increases observed at doses as low as 1 μg/mL under high X-ray exposure[3].

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

    Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay[3]

    Cell Line: B16-BL6 mouse melanoma cells
    Concentration: 0.1-100 μg/mL
    Incubation Time: 2, 4, 8, 12, 24 h
    Result: Induced time- and concentration-dependent accumulation of porphyrins (predominantly PpIX) in B16-BL6 mouse melanoma cells in vitro, with levels reaching ~9×10-8 μg/cell at 10 μg/mL after 24 h and ~5×10-7 μg/cell at 100 μg/mL after 24 h.
    In Vivo

    Hydrochloride of 5-Aminolevulinic acid (10 mg/kg/day; p.o.; daily administration; for 15 consecutive weeks) increases liver mitochondrial COX activity by 1.5-fold, COX IV protein level by 1.6-fold, and liver ATP level by 1.6-fold in female C57BL/6N mice, without inducing toxicity[1].
    Hydrochloride of 5-Aminolevulinic acid (12 mg per mouse; p.o.; daily administration; for 2 consecutive weeks) fully restores the impaired neutrophil phagocytic activity and reactive oxygen species production in 5-ALA-deficient Alas1± mice to wild-type levels[2].
    Hydrochloride of 5-Aminolevulinic acid (50 mg/kg; topical administration) significantly enhances the tumor inhibitory effect in the mouse B16-BL6 melanoma model, with no systemic toxicity observed[3].

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

    Animal Model: C57BL/6N mice (female, 6 weeks old)[1]
    Dosage: 10 mg/kg/day
    Administration: p.o.; daily; 15 weeks
    Result: Increased hepatic mitochondrial cytochrome c oxidase (COX) activity to 1.5-fold higher than control levels (P < 0.05).
    Increased hepatic COX IV protein levels to 1.6-fold higher than control levels.
    Increased hepatic ATP levels to 1.6-fold higher than control levels.
    Caused no mortality or significant body weight changes.
    Animal Model: Alas1± mice with Innate immune dysfunction (male, 22-28 weeks, generated by crossbreeding to BDF1 (F1 hybrid of C57BL/6 and DBA2))[2]
    Dosage: 12 mg per mouse daily
    Administration: p.o.; daily; 2 weeks
    Result: Partially restored peripheral blood neutrophil phagocytic activity to near wild-type levels after 1 week of administration.
    Fully restored peripheral blood neutrophil phagocytic activity to wild-type levels after 2 weeks of administration.
    Fully restored peripheral blood neutrophil reactive oxygen species (ROS) production to wild-type levels after 2 weeks of administration.
    Molecular Weight

    167.59

    Formula

    C5H10ClNO3

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)CCC(CN)=O.[H]Cl

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 250 mg/mL (1491.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 16.67 mg/mL (99.47 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 5.9669 mL 29.8347 mL 59.6694 mL
    5 mM 1.1934 mL 5.9669 mL 11.9339 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * 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.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    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 (12.41 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 (12.41 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 (596.69 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).
    Purity & Documentation

    Purity: 99.61%

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 5.9669 mL 29.8347 mL 59.6694 mL 149.1736 mL
    5 mM 1.1934 mL 5.9669 mL 11.9339 mL 29.8347 mL
    10 mM 0.5967 mL 2.9835 mL 5.9669 mL 14.9174 mL
    15 mM 0.3978 mL 1.9890 mL 3.9780 mL 9.9449 mL
    20 mM 0.2983 mL 1.4917 mL 2.9835 mL 7.4587 mL
    25 mM 0.2387 mL 1.1934 mL 2.3868 mL 5.9669 mL
    30 mM 0.1989 mL 0.9945 mL 1.9890 mL 4.9725 mL
    40 mM 0.1492 mL 0.7459 mL 1.4917 mL 3.7293 mL
    50 mM 0.1193 mL 0.5967 mL 1.1934 mL 2.9835 mL
    60 mM 0.0994 mL 0.4972 mL 0.9945 mL 2.4862 mL
    80 mM 0.0746 mL 0.3729 mL 0.7459 mL 1.8647 mL
    DMSO 100 mM 0.0597 mL 0.2983 mL 0.5967 mL 1.4917 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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    Product Name:
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