Cat. No.: HY-B0464

Hydralazine hydrochloride

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGE_E2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride 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.

Purity: 99.97%
CAS No.: 304-20-1
Formula: C₈H₉ClN₄
Molecular Weight:196.64

Storage:

4°C, sealed storage, away from moisture

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

Hydralazine hydrochloride Chemical Structure

CAS No.: 304-20-1

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

Bcl-2

Bcl-xL

Caspase-8

Caspase-9

Caspase 3

All NO Synthase Isoforms :

All DNA Methyltransferase Isoforms :

All COX Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	EC₅₀	0.45 μM Compound: Hydralazine Hydrochloride	Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis	[PMID: 20966043]

In Vitro

Hydralazine hydrochloride (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 hydrochloride (10 μM; 24 hours) reduces DNMT1 and DNMT3a mRNA expression in MCF-7 breast cancer cells^[1].
Hydralazine hydrochloride (0.1-10.0 mM) does not impair phagocytic function or viability of thioglycollate-prestimulated rat peritoneal macrophages^[2].
Hydralazine hydrochloride (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 ± 0.03 mM^[2].
Hydralazine hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride (≤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.

Cell Viability Assay^[1]

Cell Line:

Human peritoneal mesothelial cell (HPMC)
Concentration:

3μg/mL, 6 μg/mL, 12 μg/mL, 25 μg/mL, 50 μg/mL, 100 μg/mL
Incubation Time:

5 days
Result:

Caused a dose-dependent inhibition of HPMC growth.

Apoptosis Analysis^[3]

Cell Line:

Jurkat, CEM-6, MOLT-4
Concentration:

40 μM, 80 μM, 200 μM, 400 μM, 600 μM
Incubation Time:

16 h, 24 h, 48 h
Result:

Observed significant apoptosis in Jurkat and MOLT-4 cells at concentrations of 200 μM.
Induced a slight decrease in DNMT1 protein expression at 24 hr and nearly a complete loss after 48 hr.
Observed proteolytic processing of the initiator caspases-8 and -9, as well as cleavage of the effector caspase-3.
Resulted in generation of ROS and disruption of ΔΨm in Jurkat cells.
Observed that overexpression of Bcl-2 and Bcl-xL proteins prevented cell death.

In Vivo

Hydralazine hydrochloride (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 hydrochloride (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) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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:

Spinal cord injury mice^[4]
Dosage:

5 mg/kg
Administration:

Intraperitoneal injection (i.p.)
Result:

Improved not only motor function and hypersensitivity but also spontaneous pain and emotion response in SCI mice.
Inhibited both of BMDM recruitment and acrolein accumulation in the lesion epicenter of spinal cord in mice.

Animal Model:

Spontaneously hypertensive rats (SHR)^[5]
Dosage:

14 mg/kg
Administration:

Supplemented in drinking water
Result:

Reduced systolic blood pressure values and the number of adherent and migrating leukocytes in SHR.
Reduce the number of adherent and migrating leukocytes in SHR.
Decreased the levels of ICAM-1 mRNA.

Chemical Information

CAS No. 304-20-1
Appearance Solid
Molecular Weight 196.64
Formula C₈H₉ClN₄
Color White to off-white
SMILES

NNC1=NN=CC2=C1C=CC=C2.Cl
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)

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 hydrochloride 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.

Solvent & Solubility

In Vitro:

H₂O : 25 mg/mL (127.14 mM; Need ultrasonic)

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

5.0854 mL

25.4272 mL

50.8544 mL

5 mM

1.0171 mL

5.0854 mL

10.1709 mL

10 mM

0.5085 mL

2.5427 mL

5.0854 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 (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.

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (421 KB)
- English - EN (421 KB)
- Français - FR (421 KB)
- Deutsch - DE (421 KB)
- Norwegian - NO (421 KB)
- Español - ES (421 KB)
- Swedish - SV (421 KB)
- Italian - IT (421 KB)
- Korean - KR (421 KB)
- Portuguese - PT (421 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O	1 mM	5.0854 mL	25.4272 mL	50.8544 mL	127.1359 mL
	5 mM	1.0171 mL	5.0854 mL	10.1709 mL	25.4272 mL
	10 mM	0.5085 mL	2.5427 mL	5.0854 mL	12.7136 mL
	15 mM	0.3390 mL	1.6951 mL	3.3903 mL	8.4757 mL
	20 mM	0.2543 mL	1.2714 mL	2.5427 mL	6.3568 mL
	25 mM	0.2034 mL	1.0171 mL	2.0342 mL	5.0854 mL
	30 mM	0.1695 mL	0.8476 mL	1.6951 mL	4.2379 mL
	40 mM	0.1271 mL	0.6357 mL	1.2714 mL	3.1784 mL
	50 mM	0.1017 mL	0.5085 mL	1.0171 mL	2.5427 mL
	60 mM	0.0848 mL	0.4238 mL	0.8476 mL	2.1189 mL
	80 mM	0.0636 mL	0.3178 mL	0.6357 mL	1.5892 mL
	100 mM	0.0509 mL	0.2543 mL	0.5085 mL	1.2714 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.

Keywords

Hydralazine hydrochloride

3 Cited Publications

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Hydralazine hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Hydralazine hydrochloride

All NO Synthase Isoforms

All DNA Methyltransferase Isoforms

All COX Isoforms

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Hydralazine hydrochloride Related Classifications

HY-B0464 Related Classifications