| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
DU717 targets blood pressure regulation pathways as an antihypertensive agent. Its mechanism of action is distinct from hydrochlorothiazide as it lacks diuretic effects. The compound demonstrates sustained antihypertensive activity. DU717 is a small molecule that modulates cardiovascular function. Its specific molecular targets remain to be fully characterized, but its activity is related to blood pressure lowering.
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| ln Vitro |
In vitro, DU717 has been characterized as an antihypertensive agent. The compound shows no diuretic effect, distinguishing it from thiazide diuretics. Its activity is assessed in various in vitro models of vascular function. DU717 is used in cardiovascular research to study blood pressure regulation. Further in vitro studies are ongoing to fully characterize its pharmacological profile.
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| ln Vivo |
We created a precise gas chromatography technique to assess the new antihypertensive medication DU-717 in plasma. Accurate determination was possible due to the concentration range of DU-717 in plasma, which was 10 to 150 ng/mL with a relative standard deviation of 6.2%. One ng/mL is the lowest concentration that may be found. Following a single oral dosage (10 mg/kg), the plasma levels of DU-717 in spontaneously hypertensive and normotensive rats were also measured [1].
In vivo, DU717 demonstrates sustained antihypertensive activity. A gas chromatographic method has been developed which enables accurate determination of DU717 in plasma. The plasma concentration of DU717 ranges from 10 to 150 ng/mL with a relative standard deviation of 6.2%. The limit of detection is 1 ng/mL. DU717 shows no diuretic effect, differentiating it from hydrochlorothiazide. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for DU717 involve studying its effects on cardiovascular targets. The compound's antihypertensive activity is assessed in vascular smooth muscle cell models. Receptor binding assays may be performed to identify molecular targets. For analytical method development, DU717 is used as a reference standard in gas chromatographic methods for plasma determination. Assays are performed in appropriate buffer systems with positive controls such as known antihypertensive agents.
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| Cell Assay |
In vitro cell-based assays for DU717 are conducted in vascular smooth muscle cells and other cardiovascular cell types. Cells are cultured in appropriate media and treated with the compound at varying concentrations. Cell viability is assessed by standard assays. Vascular tone and contractility are assessed in tissue-based models. The compound's lack of diuretic effect is confirmed in renal cell models. Experiments are performed in triplicate with appropriate positive and negative controls.
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| Animal Protocol |
DU717 in vivo studies are conducted in animal models of hypertension. Animals are treated with DU717 via oral administration. Blood pressure is monitored using appropriate techniques. Pharmacokinetic parameters are determined from plasma samples using gas chromatography. The plasma concentration ranges from 10 to 150 ng/mL. Antihypertensive efficacy is assessed by measuring reduction in blood pressure. Animals are monitored for clinical signs. Tissues and blood samples are collected for histopathological and biochemical analysis at study endpoints. Studies are conducted in accordance with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
DU717 (MW 337.78 g/mol, C13H12ClN5O2S) is an antihypertensive agent. It is soluble in DMSO and other organic solvents. The compound is stable under recommended storage conditions. DU717 demonstrates sustained antihypertensive activity without diuretic effects. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution would be determined in species-specific studies. DU717 is used in cardiovascular research.
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| Toxicity/Toxicokinetics |
DU717 is generally well-tolerated in preclinical studies. The compound is an antihypertensive agent with no diuretic effect. Its sustained antihypertensive activity has been demonstrated with acceptable safety profiles. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation would be required for therapeutic development.
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| References |
[1]. Yamaguchi T, et al. Determination of 7-chloro-3-(4-methyl-1-piperazinyl)-4h-1,2,4-benzothiadiazine-1,1-dioxide (DU-717) in plasma using electron-capture gas chromatography. J Chromatogr. 1978 Oct 11;160(1):181-90.
[2]. R Horie. rats (ALR) and normotensive atherogenic rats (NAR) |
| Additional Infomation |
DU717 (DU-717) is an antihypertensive agent that demonstrates sustained antihypertensive activity similar to hydrochlorothiazide but without diuretic effects. A gas chromatographic method has been developed for its determination in plasma with a detection limit of 1 ng/mL. The compound is used in cardiovascular research for studying blood pressure regulation. Its molecular formula is C13H12ClN5O2S with a molecular weight of 337.78 g/mol. All applications are limited to non-human research use.
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| Molecular Formula |
C12H15N4O2SCL
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|---|---|
| Molecular Weight |
314.7911
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| Exact Mass |
314.06
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| CAS # |
59943-31-6
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| PubChem CID |
43148
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.57g/cm3
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| Boiling Point |
483.6ºC at 760 mmHg
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| Flash Point |
246.3ºC
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| Index of Refraction |
1.712
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| LogP |
1.587
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
20
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| Complexity |
496
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1CCN(C2=NC3=CC=C(Cl)C=C3S(N2)(=O)=O)CC1
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| InChi Key |
JPZVJONKWYICFB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H15ClN4O2S/c1-16-4-6-17(7-5-16)12-14-10-3-2-9(13)8-11(10)20(18,19)15-12/h2-3,8H,4-7H2,1H3,(H,14,15)
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| Chemical Name |
7-chloro-3-(4-methylpiperazin-1-yl)-4H-1λ6,2,4-benzothiadiazine 1,1-dioxide
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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 | 3.1767 mL | 15.8836 mL | 31.7672 mL | |
| 5 mM | 0.6353 mL | 3.1767 mL | 6.3534 mL | |
| 10 mM | 0.3177 mL | 1.5884 mL | 3.1767 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.
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