2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Autophagy
  3. RAR/RXR Cytochrome P450 Autophagy
  4. Talarozole

Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.

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

Talarozole Chemical Structure

Talarozole Chemical Structure

CAS No. : 201410-53-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 185 In-stock
Solution
10 mM * 1 mL in DMSO USD 185 In-stock
Solid
2 mg USD 120 In-stock
5 mg USD 168 In-stock
10 mg USD 216 In-stock
50 mg USD 390 In-stock
100 mg USD 590 In-stock
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Customer Review

Based on 24 publication(s) in Google Scholar

Other Forms of Talarozole:

Talarozole Related Antibodies

Top Publications Citing Use of Products

    Talarozole purchased from MedChemExpress. Usage Cited in: PLoS Genet. 2017 Dec 11;13(12):e1007112.  [Abstract]

    Embryos raised in media containing 0.01% DMSO develop normally. 100% of embryos treated with Talarozole between 54 and 60 hpf displayed ectopic muscle projection in the second pharyngeal arch, and the intermandibularis posterior muscles overextended in 58.3% of embryos (n=64).

    Talarozole purchased from MedChemExpress. Usage Cited in: J Exp Zool B Mol Dev Evol. 2017 Sep;328(6):575-586.  [Abstract]

    Effect of R115866 on COL9A1 expression. R115866 enhances the effect of ATRA on COL9A1 expression. R115866 (1 μM) is dissolved in DMSO. Control receive the vehicle only.

    Talarozole purchased from MedChemExpress. Usage Cited in: University of Texas. August 2017.

    100% of embryos treated with Talarozole between 54 and 60 hpf displayed ectopic muscle projection in the second pharyngeal arch, and the intermandibularis posterior muscles overextended in 58.3% of embryos (n = 64).

    Talarozole purchased from MedChemExpress. Usage Cited in: Mol Pharmacol. 2016 May;89(5):560-74.  [Abstract]

    Induction of hepatic mitochondrial biogenesis genes in mice after Talarozole (TLZ) treatment compared with vehicle-treated mice. All mRNA data are presented as fold change in mRNA abundance relative to control mice. β-Actin is used as the housekeeping gene. For protein data, results are expressed as ratio of SDHA to β-actin.

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    RXRα RXRβ RXRγ

    View All Cytochrome P450 Isoform Specific Products:

    View All Isoforms
    CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.

    IC50 & Target

    CYP26

     

    In Vitro

    When HepG2 cells are cotreated with atRA and Talarozole (1 μM), 4-OH-RA and 4-oxo-RA formation is significantly decreased[2].

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

    Talarozole Related Antibodies
    In Vivo

    A maximum 84% inhibition of CYP26 activity at 0.5 hours post-dose is predicted based on Talarozole (TLZ) Cmax of 80 nM and a Ki of 1 nM following a single dose of Talarozole. Due to the short Talarozole half-life (2.2 hrs) CYP26 activity is predicted to return to 100% by 12 hours. In agreement with the predictions, atRA concentrations are increased by 82, 63 and 60% at 4 hours post-dose in the serum, liver and testes, respectively, and concentrations returned to baseline by 24 hours. Following multiple doses of Talarozole, liver CYP26 mRNA and activity are increased suggesting autoinduction of CYP26 due to increased atRA concentrations. In agreement, atRA concentrations are elevated in serum and liver at all timepoints measured. This increase in atRA concentrations is associated with increased mRNA of the mitochondrial biogenesis markers PGC-1β and NRF-1 in comparison to control mice[3].

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

    377.51

    Formula

    C21H23N5S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CCC(CC)C(C1=CC=C(NC2=NC3=CC=CC=C3S2)C=C1)N4N=CN=C4
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 33.33 mg/mL (88.29 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 2.6489 mL 13.2447 mL 26.4894 mL
    5 mM 0.5298 mL 2.6489 mL 5.2979 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • 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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2 mg/mL (5.30 mM); Suspended solution

      This protocol yields a suspended solution of ≥ 2 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 2 mg/mL (5.30 mM); Clear solution

      This protocol yields a clear solution of ≥ 2 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 (20.0 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).
    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: 99.61%

    COA (256 KB) LCMS (121 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    Human liver microsomes (0.2 mg/mL) are incubated with 4-OH-atRA (500 nM) and NADPH, NADP+ or NAD+ (each at 2 mM) in 100 mM KPi buffer pH 7.4. In addition, 4-OH-atRA is incubated with human liver microsomes in the presence and absence of Talarozole (1 μM), a CYP26A1 specific inhibitor, and Ketoconazole (10 μM) a pan-P450 inhibitor and with NADPH as a cofactor. Following a 5 min pre-incubation, the reactions are initiated with the addition of cofactor and incubated for 30 minutes. At 30 min the reactions are quenched with equal volume of Acetonitrile and centrifuged at 3,000 g for 15 min. The supernatants are collected and 4-oxo-atRA formation is analyzed by LC-MS/MS. All incubations are normalized to a no cofactor control[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Mice[3]
    Talarozole is administered to mice as a single dose (2.5 mg/kg) or as multiple doses for three days. Serum Talarozole concentrations and serum, liver and testes atRA concentrations are measured by LC-MS/MS. Inhibition of CYP26 and changes inatRA concentrations in each tissue are predicted based on CYP26 activity in vitro and Talarozole disposition. Markers of fatty acid oxidation in the liver and spermatogonial differentiation in the testes are measured following Talarozole treatment.

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6489 mL 13.2447 mL 26.4894 mL 66.2234 mL
    5 mM 0.5298 mL 2.6489 mL 5.2979 mL 13.2447 mL
    10 mM 0.2649 mL 1.3245 mL 2.6489 mL 6.6223 mL
    15 mM 0.1766 mL 0.8830 mL 1.7660 mL 4.4149 mL
    20 mM 0.1324 mL 0.6622 mL 1.3245 mL 3.3112 mL
    25 mM 0.1060 mL 0.5298 mL 1.0596 mL 2.6489 mL
    30 mM 0.0883 mL 0.4415 mL 0.8830 mL 2.2074 mL
    40 mM 0.0662 mL 0.3311 mL 0.6622 mL 1.6556 mL
    50 mM 0.0530 mL 0.2649 mL 0.5298 mL 1.3245 mL
    60 mM 0.0441 mL 0.2207 mL 0.4415 mL 1.1037 mL
    80 mM 0.0331 mL 0.1656 mL 0.3311 mL 0.8278 mL
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    Talarozole 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:

    Talarozole201410-53-9R115866R 115866R-115866RAR/RXRCytochrome P450AutophagyRetinoic acid receptorsRetinoid X receptorsCYPsInhibitorinhibitorinhibit

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