2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. Idoxifene

Idoxifene (CB7432) is a novel tissue-specific selective estrogen receptor modulator (SERM).

For research use only. We do not sell to patients.

Idoxifene Chemical Structure

Idoxifene Chemical Structure

CAS No. : 116057-75-1

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Idoxifene Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Idoxifene (CB7432) is a novel tissue-specific selective estrogen receptor modulator (SERM).

IC50 & Target

Estrogen receptor[1]
In Vitro

Idoxifene possesses the protective roles in vascular smooth muscle cells by its blunting the angiotensin II-induced production of reactive oxygen species (ROS). Idoxifene evidently suppresses HSC activation, inhibits culture-activated HSC proliferation in a dose-dependent manner, and induces culture-activated HSC apoptosis in a time-dependent manner[1]. Idoxifene acts in bone as an estrogen agonist for osteoblasts, and shows negligible agonist activity in human endometrial cells. Idoxifene and E2 protect hepatocytes from inflammatory cell injury by inhibiting activation of the NF-κB proinflammatory transcription factor[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Idoxifene Related Antibodies
In Vivo

Animals receive daily intraperitoneal injections of Estradiol (0.5 mg/kg) and an oral gavage of Idoxifene (0.02, 0.1, and 0.5 mg/kg) for 3 days after Dimethylnitrosamine (DMN) treatment. The blood levels of LDH and Estradiol (E2) and histological grades (scores 0 to 5) of liver zone 3 necrosis are evaluated. Idoxifene at doses of over 0.1 mg/kg significantly reduces the hepatic levels of collagen and MDA in the DMN model in a dose-dependent manner. Although Idoxifene and E2 are administered by different routes, i.e., by oral ingestion and intraperitoneal injection, respectively, the antifibrotic effect of a dose of 0.5 mg/kg of Idoxifene is somewhat greater than that of the same dose of E2[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

523.45

Formula

C28H30INO
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCN3CCCC3)C=C2)\C4=CC=C(I)C=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (95.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (9.55 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Cell Assay
[1]

DNA synthesis in cultured HSCs is measured using a Cell Proliferation Biotrack ELISA system. HSCs are cultured in DMEM supplemented with 10% FBS in 96-well plate for 4 d. In the period, the medium is replaced every other day. After 4 d, the culture medium is removed and the same medium with or without 1, 10, or 100 nM of Idoxifene is added to the cells respectively. After the cells are cultured for an additional 24 h, bromodeoxyuridine (BrdU) is added into each well at a final concentration of 10 μM and the cells are incubated with BrdU for 24 h. The incorporated BrdU is detected[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Rats[2]
Adult male Wistar rats weighing about 200 g are used for the DMN model of hepatic fibrosis. The animals (n=6 in each group), which comprise groups 2 through 6 are administered a single intraperitoneal injection of 40 mg/kg DMN, diluted with saline. The controls in group 1 (n=6) receive a single dose of saline. The rats in groups 4, 5, and 6 receive daily oral gavage of Idoxifene, in a dosing vehicle (1% methylcellulose) of 10 mL/kg at a dose of 0.02, 0.1, and 0.5 mg/kg/day, respectively, for 14 days after a single injection of DMN. Idoxifene is dissolved in vehicle at a dose of 10 mg/mL as a stock solution. The animals in group 3 receive intraperitoneal injections of Estradiol valerate in olive oil at a dose of 0.5 mg/kg/day, for 14 days after the DMN injection. The animals in group 2 receive vehicle only. Animals are anesthetized with 40 mg/kg sodium pentobarbital either 0, 3, 9, or 14 days after DMN injection, and sacrificed. Blood samples are drawn from the inferior vena cava for analyses of serum levels of E2 and lactate dehydrogenase (LDH), a biomarker for necrosis, and liver tissue specimens are taken for light microscopy and immunohistochemistry.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9104 mL 9.5520 mL 19.1040 mL 47.7601 mL
5 mM 0.3821 mL 1.9104 mL 3.8208 mL 9.5520 mL
10 mM 0.1910 mL 0.9552 mL 1.9104 mL 4.7760 mL
15 mM 0.1274 mL 0.6368 mL 1.2736 mL 3.1840 mL
20 mM 0.0955 mL 0.4776 mL 0.9552 mL 2.3880 mL
25 mM 0.0764 mL 0.3821 mL 0.7642 mL 1.9104 mL
30 mM 0.0637 mL 0.3184 mL 0.6368 mL 1.5920 mL
40 mM 0.0478 mL 0.2388 mL 0.4776 mL 1.1940 mL
50 mM 0.0382 mL 0.1910 mL 0.3821 mL 0.9552 mL
60 mM 0.0318 mL 0.1592 mL 0.3184 mL 0.7960 mL
80 mM 0.0239 mL 0.1194 mL 0.2388 mL 0.5970 mL
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Idoxifene Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Idoxifene116057-75-1CB7432CB 7432CB-7432Estrogen Receptor/ERRInhibitorinhibitorinhibit

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