Idoxifene (Synonyms: CB7432)

Cat. No.: HY-U00178 Purity: 99.79%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 116057-75-1

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 230	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 230	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1300	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2200	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Estrogen Receptor/ERR Isoform Specific Products:

View All Isoforms

Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

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]

Cellular Effect

Cell Line	Type	Value	Description	References
HL-60	IC₅₀	7.7 μg/mL Compound: Idoxifene	Growth inhibition of human HL60 cells after 4 hrs by MTT assay Growth inhibition of human HL60 cells after 4 hrs by MTT assay	[PMID: 17904372]

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.

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.

116057-75-1

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
10 mM	0.1910 mL	0.9552 mL	1.9104 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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)

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

Purity: 99.79%

Select Batch:

Data Sheet (276 KB) SDS (252 KB)

COA (247 KB) HNMR (455 KB) LCMS (120 KB)

Handling Instructions (2659 KB)

References

[1]. Zhou YJ, et al. Inhibitory effects of idoxifene on hepatic fibrosis in rats. Acta Pharmacol Sin. 2005 May;26(5):581-6. [Content Brief]

[2]. Lu G, et al. Antioxidant and antiapoptotic activities of idoxifene and estradiol in hepatic fibrosis in rats. Life Sci. 2004 Jan 2;74(7):897-907. [Content Brief]

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	[1]. Zhou YJ, et al. Inhibitory effects of idoxifene on hepatic fibrosis in rats. Acta Pharmacol Sin. 2005 May;26(5):581-6. [Content Brief] [2]. Lu G, et al. Antioxidant and antiapoptotic activities of idoxifene and estradiol in hepatic fibrosis in rats. Life Sci. 2004 Jan 2;74(7):897-907. [Content Brief]

Complete Stock Solution Preparation Table

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

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

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks