| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Mineralocorticoid Receptor (MR) and Androgen Receptor (AR). Spironolactone-d7 is an internal standard and is not used for its pharmacological activity. However, its parent compound, Spironolactone, is a potent and orally active aldosterone antagonist with an IC50 of 24 nM for the MR and 77 nM for the AR.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers for quantification throughout the drug development process. Due to its potential to alter the pharmacokinetic and metabolic characteristics of medications, deuteration has drawn attention[1].
No significant in vitro activity. As a deuterium-labeled internal standard, Spironolactone-d7 is not used for inducing a pharmacological effect or inhibiting a biological target. Its purpose is to provide a chemically identical but mass-shifted analog of Spironolactone for accurate quantification. Its inert nature ensures it does not interfere with the bioanalytical assay. |
| ln Vivo |
No significant in vivo activity. Spironolactone-d7 is not intended for therapeutic or pharmacological studies. When administered, it follows the same pharmacokinetic profile as the non-deuterated drug, making it a perfect tracer in animal studies for determining the absorption, distribution, metabolism, and excretion of Spironolactone, without producing additional biological effects.
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| Enzyme Assay |
Non-cell-based: Not applicable for this use-case. Spironolactone-d7 is used as an internal standard in LC-MS/MS to calibrate the detection of the parent compound. A standard curve is generated with known ratios of unlabeled to labeled compound to quantify the unlabeled drug in unknown biological samples.
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| Cell Assay |
Cell-based assays are not directly applicable. For in vitro metabolism studies, Spironolactone-d7 can be spiked into hepatocyte incubations or microsomal reactions. The ratio of the parent compound to its deuterated standard is monitored by LC-MS/MS to measure the rate of metabolism. This allows for accurate pharmacokinetic parameter determination in a cellular context.
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| Animal Protocol |
Spironolactone-d7 is typically dosed orally or intravenously to rodents or other animals. Blood samples are collected over a time course (0-24 h or 48 h). The plasma is processed, and the concentration of unlabeled Spironolactone is determined by comparing the peak area ratio of Spironolactone/Spironolactone-d7 (the internal standard) against a known standard curve using LC-MS/MS.
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| ADME/Pharmacokinetics |
Spironolactone-d7 is a stable isotope-labeled compound and is not intended for therapeutic PK studies. Its PK properties are identical to the non-labeled drug. Spironolactone has an oral bioavailability of approximately 60-90% in humans, is extensively metabolized, and has a half-life of about 1.6 hours, with active metabolites having longer half-lives (13-18 h). The -d7 version is used as an internal standard for accurate PK analysis.
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| Toxicity/Toxicokinetics |
Spironolactone-d7 is intended for research use only and is not for human therapeutic use. The non-labeled parent drug, Spironolactone, has known clinical toxicities including hyperkalemia, gynecomastia, menstrual irregularities, and gastrointestinal disturbances. However, as an analytical standard used in minute quantities, Spironolactone-d7 poses minimal direct health risk under standard laboratory safety protocols.
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| References |
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| Additional Infomation |
Spironolactone-d7 (SC9420-d7) is an internal standard used exclusively for research. It is not an active drug and has no therapeutic or diagnostic application. The purpose of this compound is to enhance the accuracy and precision of bioanalytical methods during drug development and preclinical studies. It is supplied as a high-purity solid (>98%) and should be stored at -20degC, protected from light and moisture.
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| Molecular Formula |
C24H25D7O4S
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|---|---|
| Molecular Weight |
423.62
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| Related CAS # |
Spironolactone;52-01-7
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| Appearance |
White to off-white solid powder
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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 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3606 mL | 11.8030 mL | 23.6061 mL | |
| 5 mM | 0.4721 mL | 2.3606 mL | 4.7212 mL | |
| 10 mM | 0.2361 mL | 1.1803 mL | 2.3606 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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