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250mg | ||
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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].
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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. |
Molecular Formula |
C8H15N5O
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Molecular Weight |
197.24
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CAS # |
64000-73-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CC(CNCC1=CC=C(NN)N=N1)O
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HS Tariff Code |
2934.99.9001
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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)
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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
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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
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400  (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.
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.
(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.