| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
Androgen receptor (AR) - as an inactive metabolite, Enzalutamide carboxylic acid does not bind to the AR with significant affinity. The deuterium‑labeled form has no biological activity.
|
|---|---|
| ln Vitro |
Enzalutamide carboxylic acid‑d6 has no independent in vitro activity as it is an inactive metabolite and an internal standard. The non‑labeled Enzalutamide carboxylic acid is an inactive metabolite of Enzalutamide, resulting from amide hydrolysis, and does not contribute to the anti‑androgenic effect of the parent drug.
|
| ln Vivo |
This compound has no independent in vivo activity. It is used as an analytical standard to quantify the inactive metabolite Enzalutamide carboxylic acid in pharmacokinetic studies. Accurate measurement of this metabolite helps in understanding the metabolic clearance pathways of Enzalutamide and in assessing overall drug exposure.
|
| Enzyme Assay |
General cell‑free protocol for using Enzalutamide carboxylic acid‑d6 as an internal standard: A fixed concentration of Enzalutamide carboxylic acid‑d6 (e.g., 50‑100 ng/mL) is added to plasma or tissue samples. Samples are processed by protein precipitation with acetonitrile or by SPE. The extract is analyzed by LC‑MS/MS in negative or positive electrospray ionization mode. The m/z transitions for the analyte and the deuterated internal standard are monitored, and the peak area ratio is used for quantification.
|
| ADME/Pharmacokinetics |
General PK protocol using Enzalutamide carboxylic acid‑d6 as an internal standard: Plasma samples from Enzalutamide‑treated patients or animals are collected at various time points. A fixed concentration of Enzalutamide carboxylic acid‑d6 is added to each sample. After protein precipitation, the supernatant is analyzed by LC‑MS/MS. The concentration of Enzalutamide carboxylic acid is calculated, and PK parameters (Cmax, Tmax, AUC, t1/2) are determined from the concentration‑time profile.
|
| References | |
| Additional Infomation |
Enzalutamide carboxylic acid‑d6 has a molecular formula of C20H7D6F4N3O3S and a molecular weight of 457.43 g/mol. It is also known as MDV3100 carboxylic acid‑d6. The compound is an inactive metabolite of Enzalutamide, and the deuterated form serves as an essential internal standard for quantitative LC‑MS/MS analysis. It is stored as a solid at -20degC, and the solution can be stored at -80degC for up to 2 years. It appears as a white to off‑white solid.
|
| Molecular Formula |
C20H7D6F4N3O3S
|
|---|---|
| Molecular Weight |
457.43
|
| Appearance |
Solid powder
|
| Synonyms |
Enzalutamide carboxylic acid-d6; MDV3100 carboxylic acid-d6
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : 125 mg/mL (273.27 mM; with sonication)
|
|---|---|
| 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 | 2.1861 mL | 10.9306 mL | 21.8613 mL | |
| 5 mM | 0.4372 mL | 2.1861 mL | 4.3723 mL | |
| 10 mM | 0.2186 mL | 1.0931 mL | 2.1861 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
