Pildralazine is a hydrazine antihypertensive vasodilator containing a free hydrazine group. Pildralazine is orally bioactive and has no apparent carcinogenicity in mouse models.

Physicochemical Properties

Molecular Formula	C8H15N5O
Molecular Weight	197.2376
Exact Mass	197.128
CAS #	64000-73-3
Related CAS #	56393-22-7 (di-hydrochloride)
PubChem CID	68829
Appearance	Typically exists as solid at room temperature
LogP	-0.4
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	4
Heavy Atom Count	14
Complexity	168
Defined Atom Stereocenter Count	0
SMILES	CC(CN(C)C1=NN=C(C=C1)NN)O
InChi Key	KYIAWOXNPBANEW-UHFFFAOYSA-N
InChi Code	InChI=1S/C8H15N5O/c1-6(14)5-13(2)8-4-3-7(10-9)11-12-8/h3-4,6,14H,5,9H2,1-2H3,(H,10,11)
Chemical Name	1-[(6-hydrazinylpyridazin-3-yl)-methylamino]propan-2-ol
HS Tariff Code	2934.99.9001
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)

Biological Activity

ln Vivo	A transplacental-infantile bioassay and a long-term bioassay conducted on B6C3F1 and BALB/c mice reveal no appreciable carcinogenicity of incadralazine (6-43 mg/kg; po; thrice daily)[1]. The isolated tail artery from normotensive Wistar (NW) rats is the site of action for both pildralazine and hydralazine. This receptor is sensitive to endogenous ATP and adenosine[2]. The spontaneously hypertensive rats (SHR) model's inability to develop severe hypertension is markedly inhibited by incadralazine (1 mg/kg; po)[3].
Animal Protocol	Animal/Disease Models: Male and female B6C3F1 and to female balb/c (Bagg ALBino) mouse (8 weeks old)[1] Doses: 100, 200, and 400 ppm dose: 8, 20, and 40 mg/kg/day in B6C3F1 males, 8 , 22, and 43 mg/kg/day in B6C3F1 females, and 6, 15, and 34 mg/kg/day in BALB/c females, respectively Route of Administration: Oral gavage; added in the drinking water; provided for 80 weeks, and observed for 130-133 weeks age Experimental Results: Resulted over 80% of mice alive beyond 78 weeks of age.
References	[1]. Della Porta G, Dragani TA. Carcinogenicity study in mice on pildralazine, a hydralazinelike antihypertensive compound. J Cancer Res Clin Oncol. 1983;106(2):97-101. [2]. Chevillard C, et al. Interactions between hydralazine, propildazine and purines on arterial smooth muscle. Br J Pharmacol. 1981 Aug;73(4):811-7. [3]. Dorigotti L, et al. Effects of pildralazine alone and in combination on severe hypertension and cerebrovascular lesions in saline-drinking spontaneously hypertensive rats. Arzneimittelforschung. 1984;34(8):876-9.
Additional Infomation	Pildralazine is a tertiary amino compound and a dialkylarylamine.

Solubility Data

Solubility (In Vitro)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Solubility (In Vivo)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *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. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	5.0700 mL	25.3498 mL	50.6997 mL
	5 mM	1.0140 mL	5.0700 mL	10.1399 mL
	10 mM	0.5070 mL	2.5350 mL	5.0700 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.