Hydralazine HCl (Apresoline, Adrolazine , Apresrex)

Alias: Hydralazine Hydrochloride; 1-Hydrazinophthalazine; Adrolazine , Apresrex; Apresoline; Hydralazine chloride; Aiselazine; mono-Hydrochloride, Hydralazine; Nepresol

Cat No.:V0252 Purity: ≥98%

COA Product Data Instructions for use SDS

Hydralazine HCl (Apresoline, Adrolazine , Apresrex), thehydrochloride salt of hydralazine,is a potent and direct-acting smooth muscle relaxant and vasodilatorused for the treatment of hypertension.

Hydralazine HCl (Apresoline, Adrolazine , Apresrex) Chemical Structure CAS No.: 304-20-1
Product category: HIF HIF Prolyl-Hydroxylase

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of Hydralazine HCl (Apresoline, Adrolazine , Apresrex):

Hydralazine

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Top Publications Citing lnvivochem Products

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J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

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Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Hydralazine HCl (Apresoline, Adrolazine , Apresrex), the hydrochloride salt of hydralazine, is a potent and direct-acting smooth muscle relaxant and vasodilator used for the treatment of hypertension. It acts as a vasodilator primarily in arteries and arterioles.

Biological Activity I Assay Protocols (From Reference)

ln Vitro

In vitro activity: Hydralazine impairs up-regulation of RAG-2 gene expression and reduces secondary Ig gene rearrangements. Hydralazine subverts B lymphocyte tolerance to self and contributes to generation of pathogenic autoreactivity by disrupting receptor editing. Hydralazine directly scavenges free acrolein, decreasing intracellular acrolein availability and thereby suppressing macromolecular adduction. Hydralazine inhibits cross-linking if adding 30 min after commencing acrolein exposure but is ineffective if added after a 90-min delay. Hydralazine (0.1-10 mM) inhibits both extracellular and intracellular ROS production by inflammatory macrophages, by a ROS-scavenging mechanism probably affecting superoxide radical (O(2)(*-))-generation by xanthine oxidase (XO) and nicotinamide adenine dinucleotide/nicotinamide adenine dinucleotide phosphate (NADH/NADPH) oxidase. Hydralazine (0.1-10 mM) significantly reduces NO(*) generation, and this effect is attributable to an inhibition of NOS-2 gene expression and protein synthesis. Hydralazine also effectively blocks COX-2 gene expression which perfectly correlated with a reduction of protein levels and PGE(2) synthesis.

ln Vivo

Hydralazine affords strong, dose-dependent protection against the increases in plasma marker enzymes but not the hepatic glutathione depletion produced by allyl alcohol in mice.

Animal Protocol

N/A

Mice

References

Proc Natl Acad Sci U S A.2007 Apr 10;104(15):6317-22;J Pharmacol Exp Ther.2004 Sep;310(3):1003-10.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C8H8N4.HCL

Molecular Weight

196.64

CAS #

304-20-1

Related CAS #

Hydralazine;86-54-4

SMILES

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

InChi Key

ZUXNZUWOTSUBMN-UHFFFAOYSA-N

InChi Code

InChI=1S/C8H8N4.ClH/c9-11-8-7-4-2-1-3-6(7)5-10-12-8;/h1-5H,9H2,(H,11,12);1H

Chemical Name

phthalazin-1-ylhydrazine; hydrochloride

Synonyms

Hydralazine Hydrochloride; 1-Hydrazinophthalazine; Adrolazine , Apresrex; Apresoline; Hydralazine chloride; Aiselazine; mono-Hydrochloride, Hydralazine; Nepresol

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO:<1 mg/mL

Water:<1 mg/mL

Ethanol:<1 mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (10.58 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (10.58 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: 8.33 mg/mL (42.36 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C).

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03514108	Recruiting	Drug: Hydralazine Isosorbide Dinitrate Drug: Metformin Hydrochloride	Heart Failure Diabetes	Henrik Wiggers	March 1, 2018	Phase 4
NCT00607477	Terminated Has Results	Drug: Minoxidil Drug: Hydralazine	Treatment Induced Hypertension	University of Chicago	January 2008	Not Applicable
NCT02522208	Completed	Drug: BiDil XR Drug: BiDil Immediate Release (IR)	Heart Failure	Arbor Pharmaceuticals, Inc.	September 2015	Phase 1
NCT02933593	Withdrawn	Drug: Labetalol Drug: Hydralazine	Hypertension	St. Louis University	August 2016	Not Applicable

Biological Data

See this image and copyright information in PMC Fig. 1. BcR ligation induces RAG-2 and Vκ–Jκ mRNA expression in bone marrow B cells. Cells were cultured in the presence of goat anti-human IgM F(ab′)2 fragments and were harvested after 48 h of treatment. (A) RT-PCR analysis of RAG-2 and GAPDH mRNA in BM B cells from five-feature transgenic animals before and after stimulation with various concentrations of goat anti-human IgM F(ab′)2 fragments. PCR products and DNA markers were visualized by ethidium bromide staining after agarose gel electrophoresis. Control GAPDH transcript was amplified as an ubiquitously expressed gene and used to standardize loading. (B) Summary of RT-PCR analysis of RAG-2 mRNA expression levels. Relative intensity is calculated as RAG-2:GAPDH ratio of signal. (C) Cell lysates were used as template in RT-PCR assays for rearrangement products of human Vκ1, Vκ3, Vκ4, and Vκ5 gene families. Lanes show results from BM cultures treated with goat anti-human IgM F(ab′)2 fragments or medium. The control transcript CD14 was amplified as a ubiquitously expressed gene and used to standardize loading. (D) Summary of RT-PCR analysis of Vκ–Jκ5 mRNA expression levels in unstimulated (black bars) and anti-human IgM-stimulated (white bars) BM cells. Represented are the expressions (%) of each human Vκ gene family relative to the total human Vκ gene repertoire.

See this image and copyright information in PMC Fig. 2. BcR ligation induces κ → λ-chain shifting in bone marrow cells from transgenic mice. (A) BM cells from five-feature mice were cultured for 48 h with medium, goat anti-human IgM F(ab′)2 fragments, or goat anti-human κ-chain F(ab′)2 fragments. Cells were stained with anti-B220-PE and biotinylated anti-human λ-chain and analyzed on a FACScan flow cytometer. A minimum of 10,000 events was collected per sample, and data were analyzed with CellQUEST (version 3.1; Becton Dickinson). (B) Summary of FACS analysis with mean percentages of B cells expressing human λ-chain in five-feature BM cultures ±SE. ∗, P < 0.05. (C) Bone marrow cells from five-feature transgenic mice were cultured either alone or with 10 μg/ml goat anti-human IgM F(ab′)2 fragments. The absolute numbers of B220+ cells were determined at various times by counting viable cell numbers and determining the percentage of B220+ cells in flow cytometry assays.

See this image and copyright information in PMC Fig. 3. Hydralazine and a MEK inhibitor block Vκ–Jκ5 rearrangements after BcR stimulation. (A) BM cells from five-feature transgenic animals were preincubated with hydralazine or PD98059 for two hours and then stimulated with goat anti-human IgM F(ab′)2 fragments (10 μg/ml) for 48 h. Cells were harvested and analyzed by RT-PCR for Vκ1–Jκ5 and Vκ4–Jκ5 rearrangements. PCR products and DNA markers were visualized by ethidium bromide staining after agarose gel electrophoresis. (B) Summary of RT-PCR analysis of Vκ1–Jκ5 (white bars) and Vκ4–Jκ5 (gray bars) mRNA expression levels. Results are expressed relative to mean intensities obtained with vehicle (DMSO)-exposed samples for each Vκ–Jκ5 rearrangement.