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| 5mg |
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| Targets |
Triamterene D5 targets the epithelial sodium channel (ENaC), a membrane protein that mediates sodium reabsorption in the distal convoluted tubule and collecting duct of the kidney. ENaC is composed of alpha, beta, and gamma subunits and is regulated by aldosterone and other factors. By blocking ENaC in a voltage-dependent manner, Triamterene inhibits sodium reabsorption, leading to increased sodium and water excretion (diuresis) while sparing potassium. The compound is a mild diuretic with potassium-sparing properties. The deuterated D5 form is used as an analytical internal standard for quantifying Triamterene in biological samples.
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| ln Vitro |
In vitro, Triamterene (parent compound) blocks epithelial sodium channels (ENaC) in a voltage-dependent manner. The compound inhibits sodium current through ENaC channels expressed in Xenopus oocytes or mammalian cells. In cellular assays using renal epithelial cells, Triamterene reduces sodium transport and inhibits ENaC-mediated sodium reabsorption. The D5-labeled form is expected to exhibit identical in vitro activity to the parent compound, making it suitable as an internal standard for quantifying Triamterene in bioanalytical methods. The compound is used in research to study sodium channel function and diuretic mechanisms.
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| ln Vivo |
In vivo, Triamterene (parent compound) is used clinically as a potassium-sparing diuretic for the treatment of hypertension and edema. It prevents the kidneys from absorbing too much salt, allowing the salt to instead be passed in the urine. The compound is often used in combination with other diuretics (e.g., hydrochlorothiazide) to counteract potassium loss. The deuterated D5 form is used as an internal standard for pharmacokinetic studies and therapeutic drug monitoring, enabling accurate quantification of Triamterene levels in plasma and urine samples by LC-MS/MS.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Triamterene involve measuring ENaC channel activity using electrophysiological techniques. Xenopus oocytes or mammalian cells expressing ENaC subunits are used. Whole-cell patch-clamp or two-electrode voltage-clamp electrophysiology is performed to measure sodium currents. Varying concentrations of Triamterene or the D5 internal standard (0.001-100 microM) are applied, and inhibition of sodium current is measured. IC₅0 values for ENaC blockade are calculated from dose-response curves. Binding studies using radiolabeled Triamterene can also be performed to assess binding affinity to ENaC.
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| Cell Assay |
Cellular assays for Triamterene are performed using renal epithelial cell lines such as A6 (Xenopus) or mCCD (mouse cortical collecting duct) cells that express ENaC. Cells are cultured on permeable supports (Transwell inserts) to form polarized monolayers. Cells are treated with serial dilutions of Triamterene (0.001-100 microM) for 1-24 hours. Transepithelial sodium transport is measured by short-circuit current (Isc) in Ussing chambers. Intracellular sodium levels are measured using fluorescent sodium indicators. Cell viability is assessed by MTT assay to ensure compound effects are not due to cytotoxicity. IC₅0 values for inhibition of sodium transport are calculated.
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| Animal Protocol |
In vivo animal studies for Triamterene are conducted in rodent models to study diuretic effects and pharmacokinetics. Rats or mice are administered Triamterene orally or intraperitoneally at doses of 1-20 mg/kg. Animals are placed in metabolic cages for urine collection over 24-hour periods. Urine volume, sodium excretion, potassium excretion, and creatinine clearance are measured. Blood pressure is monitored by tail-cuff plethysmography. Pharmacokinetic parameters (Cmax, Tmax, AUC, t1/2) are determined from plasma and urine samples by LC-MS/MS using the D5 internal standard.
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| ADME/Pharmacokinetics |
Triamterene D5 (CAS#: 1189922-23-3) has molecular formula C12H₆D₅N₇ and molecular weight 258.29. The IUPAC name is 6-(phenyl-d5)pteridine-2,4,7-triamine. The compound is a deuterium-labeled form of Triamterene, a potassium-sparing diuretic that blocks epithelial sodium channels (ENaC). It is used as an internal standard for quantifying Triamterene in biological matrices for pharmacokinetic and metabolic studies. Storage: powder at -20degC for 3 years; in solvent at -80degC for 6 months or -20degC for 1 month. For research use only.
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| Additional Infomation |
Triamterene D5 (CAS#: 1189922-23-3) is a deuterium-labeled form of Triamterene, a potassium-sparing diuretic used primarily to treat hypertension and edema. Triamterene blocks the epithelial sodium channel (ENaC) in a voltage-dependent manner, inhibiting sodium reabsorption in the distal nephron and promoting diuresis while sparing potassium. The D5-labeled analog is used as an internal standard in LC-MS/MS bioanalytical methods for pharmacokinetic studies, therapeutic drug monitoring, and clinical research. For research use only, not for human therapeutic applications.
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| Molecular Formula |
C12H6D5N7
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|---|---|
| Molecular Weight |
258.29300
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| Exact Mass |
258.139
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| CAS # |
1189922-23-3
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| Related CAS # |
Triamterene;396-01-0
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| PubChem CID |
45040581
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.577
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
19
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| Complexity |
307
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[2H]C1=C(C(=C(C(=C1[2H])[2H])C2=NC3=C(N=C(N=C3N=C2N)N)N)[2H])[2H]
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| InChi Key |
FNYLWPVRPXGIIP-RALIUCGRSA-N
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| InChi Code |
InChI=1S/C12H11N7/c13-9-7(6-4-2-1-3-5-6)16-8-10(14)18-12(15)19-11(8)17-9/h1-5H,(H6,13,14,15,17,18,19)/i1D,2D,3D,4D,5D
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| Chemical Name |
6-(2,3,4,5,6-pentadeuteriophenyl)pteridine-2,4,7-triamine
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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 | 3.8716 mL | 19.3581 mL | 38.7162 mL | |
| 5 mM | 0.7743 mL | 3.8716 mL | 7.7432 mL | |
| 10 mM | 0.3872 mL | 1.9358 mL | 3.8716 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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