Cat. No.: HY-B0464A

Hydralazine

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

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 PGE_E2; 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.

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Pureté: 99.94%
CAS No.: 86-54-4
Formule: C₈H₈N₄
Masse moléculaire:160.18

Stockage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Hydralazine Chemical Structure

CAS No.: 86-54-4

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
- Essai clinique
Chemical Information
Publications (3)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

COX-2

iNOS

Voir tous les produits spécifiques à Isoform DNA Methyltransferase :

Voir tous les produits spécifiques à Isoform COX :

Voir tous les produits spécifiques à Isoform NO Synthase :

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/IFN^γ-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.

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 86-54-4
Appearance Solid
Masse moléculaire 160.18
Formule C₈H₈N₄
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (3)

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Journal Impact Factor

J Pharm Anal

Hydralazine represses Fpn ubiquitination to rescue injured neurons via competitive binding to UBA52. [Abstract]

2024 Jan;14(1):86-99. PMID: 38352945
Neurosci Bull

Acrolein Aggravates Secondary Brain Injury After Intracerebral Hemorrhage Through Drp1-Mediated Mitochondrial Oxidative Damage in Mice. [Abstract]

2020 Oct;36(10):1158-1170. PMID: 32436179

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.
Microchem J

2025 Nov 24;220:116331.

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

6.2430 mL

31.2149 mL

62.4298 mL

5 mM

1.2486 mL

6.2430 mL

12.4860 mL

10 mM

0.6243 mL

3.1215 mL

6.2430 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
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μL
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
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%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (289 KB)
SDS (394 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
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OR (2659 KB)
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Instruction de manipulation (2659 KB)

Références

[1]. Arce C, et al. Hydralazine target: from blood vessels to the epigenome. J Transl Med. 2006;4:10. Published 2006 Feb 28. [Content Brief]

[2]. Leiro JM, et al. Antioxidant activity and inhibitory effects of hydralazine on inducible NOS/COX-2 gene and protein expression in rat peritoneal macrophages. Int Immunopharmacol. 2004;4(2):163-177. [Content Brief]

[3]. de Flora S, et al. In vivo and in vitro genotoxicity of three antihypertensive hydrazine derivatives (hydralazine, dihydralazine, and endralazine). Environ Mutagen. 1982;4(5):605-619. [Content Brief]

[4]. Park J, et al. Neuroprotective role of hydralazine in rat spinal cord injury-attenuation of acrolein-mediated damage. J Neurochem. 2014;129(2):339-349. [Content Brief]

[5]. Bai L, et al. Attenuation of mouse somatic and emotional inflammatory pain by hydralazine through scavenging acrolein and inhibiting neuronal activation. Pain Physician. 2012;15(4):311-326. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Hydralazine

3 Cited Publications

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Hydralazine

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Publications Citing Use of MedChemExpress (MCE) Hydralazine

Voir tous les produits spécifiques à Isoform DNA Methyltransferase

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Activité biologique

Chemical Information

Publications (3)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Hydralazine Related Classifications

HY-B0464A Related Classifications