| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
Epitizide targets the Na-Cl cotransporter (NCC) in the distal convoluted tubule of the kidney, inhibiting sodium and chloride reabsorption, leading to increased urine production. It is often used in fixed-dose combination with triamterene (50 mg/4 mg) for potassium-sparing effects.
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|---|---|
| ln Vitro |
In vitro assays using oocytes expressing the human NCC transporter confirm thiazide diuretic activity. Epitizide (1-100 uM) inhibits NCC-mediated sodium uptake in a concentration-dependent manner, with potency comparable to other thiazide diuretics like hydrochlorothiazide.
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| ln Vivo |
In animal models (rats, dogs), oral administration of Epitizide (0.1-5 mg/kg) induces diuresis and natriuresis, increasing urine volume and urinary sodium excretion within 2-4 hours post-dose. It reduces blood pressure in hypertensive models when administered chronically (1-4 weeks).
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| Enzyme Assay |
This cell-free binding assay is performed using membrane preparations from cells overexpressing human NCC. Membranes (50-100 ug protein) are incubated with 3H-metolazone (1-10 nM) and varying concentrations of Epitizide (0.1 nM - 100 uM) in binding buffer for 60 min at room temperature. Bound radioactivity is collected by rapid filtration. Ki values are calculated from competition binding curves.
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| Cell Assay |
Cells stably expressing human NCC (e.g., HEK293-NCC cells) are seeded in 96-well plates. Cells are incubated with sodium-sensitive dye (SBFI-AM) for 30 min. After washing, cells are treated with Epitizide (1-100 uM) for 15 min, then sodium influx is stimulated with benzamil. Fluorescence (Ex/Em 340/380 nm) is measured to assess NCC inhibition.
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| Animal Protocol |
Normotensive or hypertensive rats (e.g., SHR, DOCA-salt) are fasted overnight, then Epitizide is administered orally by gavage at 0.5-5 mg/kg. After dosing, animals are placed in metabolic cages for 6-24 hours. Urine volume, urinary sodium, potassium, and chloride concentrations are measured. Blood pressure is measured by tail-cuff or telemetry 2-8 hours post-dose for acute effects, or daily for 2-4 weeks for chronic effects.
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| ADME/Pharmacokinetics |
Following oral administration, Epitizide is absorbed with peak plasma concentrations within 2-4 hours. It is protein-bound (~90%) and has a terminal half-life of 8-12 hours. Metabolism occurs via hepatic CYP enzymes, with renal excretion of metabolites. Bioavailability is approximately 50-70%. Contraindicated in eGFR <30 mL/min/1.73 m2.
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| Toxicity/Toxicokinetics |
Standard thiazide diuretic toxicity applies. Hypokalemia, hyperuricemia, and glucose intolerance may occur at higher doses. Contraindicated in severe renal impairment and sulfonamide allergy. Long-term use requires monitoring of electrolytes, uric acid, and blood glucose. Epitizide is not approved in some regions.
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| Additional Infomation |
Epitizide is a benzothiadiazine drug. Epitizide is a diuretic, often used in combination with triamterene. Epitizide is a benzothiadiazine sulfonamide derivative containing a trifluoroethylthio group, belonging to the thiazide diuretic class.
This is a pharmaceutical diuretic, approved in some countries for clinical use in combination with triamterene (50 mg/4 mg fixed-dose ratio). It is a research-grade reference standard for diuretic method development (HPLC-UV, doping control, forensic toxicology). Molecular formula: C10H11ClF3N3O4S3; molecular weight: 425.86. |
| Molecular Formula |
C10H11CLF3N3O4S3
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|---|---|
| Molecular Weight |
425.86
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| Exact Mass |
424.955
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| CAS # |
1764-85-8
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| PubChem CID |
15671
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.636g/cm3
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| Boiling Point |
586.6ºC at 760mmHg
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| Flash Point |
308.6ºC
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| Vapour Pressure |
9.64E-14mmHg at 25°C
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| Index of Refraction |
1.566
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| LogP |
4.641
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
662
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=CC2NC(CSCC(F)(F)F)NS(=O)(=O)C=2C=C1S(N)(=O)=O
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| InChi Key |
RINBGYCKMGDWPY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H11ClF3N3O4S3/c11-5-1-6-8(2-7(5)23(15,18)19)24(20,21)17-9(16-6)3-22-4-10(12,13)14/h1-2,9,16-17H,3-4H2,(H2,15,18,19)
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| Chemical Name |
6-chloro-1,1-dioxo-3-(2,2,2-trifluoroethylsulfanylmethyl)-3,4-dihydro-2H-1λ6,2,4-benzothiadiazine-7-sulfonamide
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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 | 2.3482 mL | 11.7409 mL | 23.4819 mL | |
| 5 mM | 0.4696 mL | 2.3482 mL | 4.6964 mL | |
| 10 mM | 0.2348 mL | 1.1741 mL | 2.3482 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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