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Idoxifene

Cat No.:V6794 Purity: ≥98%
Idoxifene (CB7432) is a tissue-specific selective estrogen receptor modulator (SERM).
Idoxifene
Idoxifene Chemical Structure CAS No.: 116057-75-1
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
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Product Description
Idoxifene (CB7432) is a tissue-specific selective estrogen receptor modulator (SERM).
Biological Activity I Assay Protocols (From Reference)
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].
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].
References

[1]. Inhibitory effects of idoxifene on hepatic fibrosis in rats. Acta Pharmacol Sin. 2005 May;26(5):581-6.

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

Additional Infomation
Idoxifene is a stilbenoid.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
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 Data
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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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