| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg | |||
| Other Sizes |
| Targets |
Idoxifene targets the estrogen receptor (ER), a nuclear receptor that mediates the effects of estrogen on gene transcription. As a selective estrogen receptor modulator (SERM), Idoxifene can act as either an estrogen agonist or antagonist depending on the tissue and the context. It is a close structural analog of tamoxifen. By binding to the estrogen receptor, Idoxifene modulates estrogen-dependent gene expression, which underlies its potential therapeutic effects in conditions such as breast cancer and other estrogen-related disorders.
|
|---|---|
| ln Vitro |
By reducing the generation of reactive oxygen species (ROS) brought on by angiotensin II, idoxifene protects vascular smooth muscle cells. Idoxifene causes culture-activated HSC death in a time-dependent manner, reduces HSC activation considerably, and decreases culture-activated HSC growth in a dose-dependent manner [1]. Idoxifene exhibits very little agonist action in human endometrial cells but functions as an estrogen agonist for osteoblasts in bone. By preventing the activation of the pro-inflammatory transcription factor NF-κB, idoxifene and E2 shield hepatocytes from damage caused by inflammatory cells [2].
In vitro, Idoxifene is a nonsteroidal SERM that binds to the estrogen receptor. Its activity is typically measured using receptor binding assays and functional assays such as reporter gene assays in cells expressing the estrogen receptor. The compound's ability to modulate estrogen-dependent gene expression has been confirmed in vitro. Its close structural similarity to tamoxifen suggests that it may have similar pharmacological properties. However, specific in vitro data, such as IC50 or EC50 values, are not detailed in standard product descriptions. |
| ln Vivo |
Animals were given daily intraperitoneal injections of estradiol (0.5 mg/kg) and oral administration of edoxifen (0.02, 0.1, and 0.5 mg/kg) three days following dimethylnitrosamine (DMN) therapy. LDH and estradiol (E2) levels in the blood as well as the histological grade of liver zone 3 necrosis (score 0 to 5) were measured. Idedoxifene dramatically decreased liver collagen and MDA levels in the DMN model in a dose-dependent manner at dosages more than 0.1 mg/kg. Even though edoxifen and E2 are administered by oral and intraperitoneal injection, respectively, their anti-fibrotic effects are marginally greater at 0.5 mg/kg of edoxifen than they are at the same dose of E2 [2].
In vivo, Idoxifene has been investigated in clinical trials as a potential therapeutic agent. It has a maximum clinical trial phase of II. The compound has been studied for potential applications in breast cancer and other estrogen-related disorders. However, specific in vivo efficacy data, such as results from clinical trials, are not detailed in standard product descriptions. Idoxifene is a research compound that has been investigated for therapeutic use. |
| Enzyme Assay |
In vitro receptor binding assays for Idoxifene measure its affinity for the estrogen receptor. Membranes from cells expressing the estrogen receptor are incubated with a radiolabeled estrogen ligand and varying concentrations of Idoxifene. The Ki is determined from competition binding curves. Functional assays measure the compound's ability to modulate estrogen receptor-mediated transcription using reporter gene assays. Cells are transfected with an estrogen response element (ERE)-luciferase reporter and treated with Idoxifene in the presence or absence of estrogen. The modulation of luciferase activity is measured.
|
| Cell Assay |
In vitro cell-based assays for Idoxifene are used to study its effects on estrogen receptor signaling. Cells expressing the estrogen receptor are treated with Idoxifene, and the expression of estrogen target genes is measured by quantitative PCR. Cell proliferation assays are used to assess the compound's effects on the growth of estrogen-dependent cancer cell lines, such as MCF-7 breast cancer cells. These assays confirm the compound's activity as a SERM.
|
| Animal Protocol |
In vivo animal experiments for Idoxifene would typically be conducted in animal models of breast cancer or other estrogen-related disorders. In a typical study, mice bearing xenograft tumors of estrogen-dependent cancer cells are treated with Idoxifene, and tumor growth is monitored. The compound's ability to inhibit tumor growth is assessed. However, specific protocols for Idoxifene are not detailed in standard product descriptions. Idoxifene has been investigated in clinical trials.
|
| ADME/Pharmacokinetics |
Idoxifene has a molecular weight of 523.45 g/mol and a molecular formula of C28H30INO. It has a monoisotopic molecular weight of 523.14 Da. It is a solid compound with a purity of ≥98%. It is soluble in DMSO and other organic solvents. For storage, it is recommended to keep the powder at -20°C. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have been characterized in the context of clinical development. Idoxifene is a small molecule drug.
|
| Toxicity/Toxicokinetics |
Detailed toxicity data for Idoxifene is not provided in standard product descriptions. As a compound that has been investigated in clinical trials, its safety profile has been evaluated in human studies. However, specific toxicity data, such as adverse effects or organ toxicity, are not detailed. As a SERM, it may have effects similar to tamoxifen, including hot flashes, nausea, and an increased risk of thromboembolic events. As with all research chemicals, standard laboratory safety precautions should be followed when handling Idoxifene.
|
| References | |
| Additional Infomation |
Iodoxifene is a stilbene compound.
Idoxifene is a research compound and is not approved for clinical use in many countries. It is a nonsteroidal selective estrogen receptor modulator (SERM) belonging to the triphenylethylene class, making it a close structural analog of tamoxifen. Idoxifene has a maximum clinical trial phase of II. It has been investigated for potential therapeutic applications in breast cancer and other estrogen-related disorders. Its mechanism of action involves binding to the estrogen receptor and modulating estrogen-dependent gene expression. Idoxifene is a valuable research tool for studying estrogen receptor pharmacology and SERM biology. |
| Molecular Formula |
C28H30NOI
|
|---|---|
| Molecular Weight |
523.4479
|
| Exact Mass |
523.137
|
| CAS # |
116057-75-1
|
| PubChem CID |
3034011
|
| Appearance |
White to off-white solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
573.4±50.0 °C at 760 mmHg
|
| Melting Point |
108-109° (McCague et al.)
|
| Flash Point |
300.6±30.1 °C
|
| Vapour Pressure |
0.0±1.6 mmHg at 25°C
|
| Index of Refraction |
1.623
|
| LogP |
9.5
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
31
|
| Complexity |
547
|
| Defined Atom Stereocenter Count |
0
|
| 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~50 mg/mL (~95.52 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (9.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9104 mL | 9.5520 mL | 19.1040 mL | |
| 5 mM | 0.3821 mL | 1.9104 mL | 3.8208 mL | |
| 10 mM | 0.1910 mL | 0.9552 mL | 1.9104 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
