2. Epigenetics NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. DNA Methyltransferase Reactive Oxygen Species (ROS) COX NO Synthase PGE synthase
  4. Hydralazine

Hydralazine is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGEE2; meanwhile, Hydralazine scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain.

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

CAS No. : 86-54-4

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
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Hydralazine:

Hydralazine Related Antibodies

Top Publications Citing Use of Products

    Hydralazine purchased from MedChemExpress. Usage Cited in: Neurosci Bull. 2020 Oct;36(10):1158-1170.  [Abstract]

    Western blots (left) and analysis (right) of cyto-Drp1, mito-Drp1, and T-Drp1 in different groups of mice. Hydralazine (acrolein scavenger) suppresses the translocation of Drp1 and alleviates the morphological disruption of mitochondria after ICH in mice.

    View All DNA Methyltransferase Isoform Specific Products:

    View All Isoforms
    DNA Methyltransferase DNMT1 DNMT3 MGMT

    View All COX Isoform Specific Products:

    View All Isoforms
    COX COX-1 COX-2 COX-3

    View All NO Synthase Isoform Specific Products:

    View All Isoforms
    nNOS iNOS eNOS

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Hydralazine is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGEE2; meanwhile, Hydralazine scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain[1][2][3][4][5].

    IC50 & Target

    COX-2

     

    iNOS

     

    Cellular Effect
    Cell Line Type Value Description References
    NHDF IC50
    > 50 μM
    Compound: 36
    Cytotoxicity against NHDF assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against NHDF assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 28671460]
    In Vitro

    Hydralazine (10 μM; 5 days) demethylates and reactivates expression of silenced tumor suppressor genes (ER, RARβ, p16) in MDA-231, MCF-7, and T24 cancer cell lines, respectively[1].
    Hydralazine (10 μM; 24 hours) reduces DNMT1 and DNMT3a mRNA expression in MCF-7 breast cancer cells[1].
    Hydralazine (0.1-10.0 mM) does not impair phagocytic function or viability of thioglycollate-prestimulated rat peritoneal macrophages[2].
    Hydralazine (0.1-10.0 mM) significantly inhibits nitrite production by LPS/IFN-γ-stimulated thioglycollate-prestimulated rat peritoneal macrophages, with an IC50 of 0.43 mM[2].
    Hydralazine (1.0-10.0 mM) inhibits both NOS-2 and COX-2 protein synthesis in LPS/IFNγ-stimulated thioglycollate-prestimulated rat peritoneal macrophages[2].
    Hydralazine (3.1-50 nmol, plate incorporation test without S-9 mix; 1 mg per plate, spot test with/without S-9 mix) is a direct-acting, low-potency mutagen that induces mixed genetic mutation mechanisms in Salmonella typhimurium strains TA1535, TA100, TA1537, TA97, and TA98, with highest potency in strain TA97[3].
    Hydralazine (5 mg per spot, spot test; serial twofold dilutions, micromethod assay with/without S-9 mix; 16 h incubation at 37°C) is a direct-acting genotoxin that is preferentially lethal to repair-deficient Escherichia coli strains WP67 and CM871, indicating involvement of recA recombination repair, lexA post-replication repair, and polA repair mechanisms, with no dependence on excision repair systems[3].
    Hydralazine (≤25 μM) significantly mitigates acrolein-mediated cell death in PC12 cells[4].

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

    Hydralazine Related Antibodies

    RT-PCR[1]

    Cell Line: MCF-7 breast cancer cells
    Concentration: 10 μM
    Incubation Time: 24 h
    Result: Decreased the mRNA expression of DNMT1 and DNMT3a, as confirmed by reduced band intensity on PCR analysis relative to untreated controls.
    Showed no change in DNMT3b mRNA expression.
    Parmacokinetics
    Species Dose Route Brain Concentration
    Mice[4] 5 mg/kg i.p. ~30 μM
    In Vivo

    Hydralazine (i.p.; daily; 7 d) promotes demethylation of the estrogen receptor gene promoter and reactivates estrogen receptor expression in MDA-MB-231 breast cancer xenografts in nude mice[1].
    Hydralazine (used in combination with valproic acid (HY-10585)) eliminates tumor recurrence of HT1080 fibrosarcoma xenografts in nude mice[1].
    Hydralazine (83 mg/kg; i.p.; once daily; 5 days) induces DNA fragmentation in the liver, kidney and spleen (but not the lung) of mice at 6 hours after the last administration, and the damage is completely repaired at 12 hours post-administration; meanwhile, it moderately increases the sister chromatid exchange rate of mouse bone marrow cells by 33%[3].
    Hydralazine (5 mg/kg; i.p.; twice; 14 d) reduces acrolein levels by 50-70% in the injured spinal cord of rats, decreases post-injury cyst formation by 70%, improves motor function recovery, and alleviates mechanical hyperalgesia in rat models of spinal cord injury[4].
    Hydralazine (0.1-10 mg/kg; i.p.; single dose) dose-dependently alleviates formalin-induced somatic and emotional inflammatory pain in male C57BL/6 mice, with a ED50 of 0.239-1.0160 mg/kg, while inhibiting excessive acrolein production and neuronal activation in the spinal cord[5].
    Hydralazine (10 mg/kg; i.p.; single dose) does not impair central nervous system function in male C57BL/6 mice[5].

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

    Animal Model: Nude mice[1]
    Dosage: equivalent to those used in hypertensive patients
    Administration: i.p.; daily; 7 days
    Result: Induced demethylation of the estrogen receptor (ER) gene promoter in xenografted tumors, which correlated with re-expression of ER mRNA and protein.
    Animal Model: Noninbred Swiss mice (male, 2-3 months old)[3]
    Dosage: 83 mg/kg (single dose); 28 mg/kg (daily x5)
    Administration: i.p.; single dose; daily for 5 consecutive days
    Result: Induced a modest but statistically significant increase in DNA elution rate in liver 6 hours post single 83 mg/kg dose.
    Induced a modest but statistically significant increase in DNA elution rate in kidney 6 hours post single 83 mg/kg dose.
    Induced a modest but statistically significant increase in DNA elution rate in spleen 6 hours post single 83 mg/kg dose.
    Showed minimal or absent DNA damage in liver, kidney, and spleen 1 hour and 12 hours post single 83 mg/kg dose.
    Showed no statistically significant DNA damage in lung at 1, 6, or 12 hours post single 83 mg/kg dose.
    Showed no statistically significant DNA damage in liver, lung, kidney, or spleen 6 hours after final daily 28 mg/kg dose (x5).
    Animal Model: Noninbred Swiss mice (male, 2-3 months old)[3]
    Dosage: 83 mg/kg
    Administration: i.p.; single dose
    Result: Induced a 33% increase in SCE frequency per diploid bone marrow cell relative to control mice, with a mean of 3.6 ± 1.8 SCEs per metaphase.
    Animal Model: Sprague-Dawley (male, 200-250 grams at surgery, spinal cord contusion injury model)[4]
    Dosage: 5 mg/kg (tissue distribution); 5 mg/kg (two doses, acrolein reduction); 5 mg/kg (daily for 14 days, cyst formation, locomotor function, mechanical allodynia)
    Administration: i.p.; single dose; two doses (immediately post-injury, 24 hours post-injury); daily; 14 days
    Result: Reached concentrations of 2.9 μg/g (≈20 μM) in spinal cord tissue and 4.4 μg/g (≈30 μM) in brain tissue at 2 hours post-single 5 mg/kg i.p.
    dose.
    Reduced acrolein levels from 31.1 arbitrary units to 8.7 arbitrary units in moderate spinal cord injury, and from 42.7 arbitrary units to 21.3 arbitrary units in severe spinal cord injury after two 5 mg/kg i.p.
    doses.
    Reduced spinal cord cyst area from 38.0% of total cord area to 11.4% at 28 days post-injury after daily 5 mg/kg i.p.
    treatment for 14 days.
    Improved BBB locomotor scores to 16.1 at 28 days post-injury (compared to 12.4 in untreated injured rats), with significant improvements detected at 7, 14, 21, and 28 days post-injury after daily 5 mg/kg i.p.
    treatment for 14 days.
    Mitigated mechanical allodynia: at 14 days post-injury, paw withdrawal threshold was 8.1 g; at 21 days post-injury, threshold was 8.1 g; at 28 days post-injury, threshold was 9.7 g (all significantly higher than thresholds in untreated injured rats) after daily 5 mg/kg i.p.
    treatment for 14 days.
    Clinical Trial
    Molecular Weight

    160.18

    Formula

    C8H8N4
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    N/N=C1NN=CC2=C\1C=CC=C2
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 20 mg/mL (124.86 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 6.2430 mL 31.2149 mL 62.4298 mL
    5 mM 1.2486 mL 6.2430 mL 12.4860 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    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 mg/mL (12.49 mM); Clear solution

      This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 mg/mL (12.49 mM); Clear solution

      This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
    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.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    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. 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
    DMSO 1 mM 6.2430 mL 31.2149 mL 62.4298 mL 156.0744 mL
    5 mM 1.2486 mL 6.2430 mL 12.4860 mL 31.2149 mL
    10 mM 0.6243 mL 3.1215 mL 6.2430 mL 15.6074 mL
    15 mM 0.4162 mL 2.0810 mL 4.1620 mL 10.4050 mL
    20 mM 0.3121 mL 1.5607 mL 3.1215 mL 7.8037 mL
    25 mM 0.2497 mL 1.2486 mL 2.4972 mL 6.2430 mL
    30 mM 0.2081 mL 1.0405 mL 2.0810 mL 5.2025 mL
    40 mM 0.1561 mL 0.7804 mL 1.5607 mL 3.9019 mL
    50 mM 0.1249 mL 0.6243 mL 1.2486 mL 3.1215 mL
    60 mM 0.1040 mL 0.5202 mL 1.0405 mL 2.6012 mL
    80 mM 0.0780 mL 0.3902 mL 0.7804 mL 1.9509 mL
    100 mM 0.0624 mL 0.3121 mL 0.6243 mL 1.5607 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Hydralazine Related Classifications

    Help & FAQs
    • 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.

    Keywords:

    Hydralazine86-54-4DNA MethyltransferaseReactive Oxygen Species (ROS)COXNO SynthasePGE synthaseDNMTsDNA MTasesCyclooxygenaseNitric oxide synthasesNOSProstaglandin E synthasecervical cancerhypertensionCOX-2arterial smooth musclebreast cancermacrophagesNOS-2ROSDNA methyltransferasetumor suppressor genesInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Hydralazine
    Cat. No.:
    HY-B0464A
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB) Italian - IT (393 KB) Korean - KR (393 KB) Portuguese - PT (393 KB)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.