1. Metabolic Enzyme/Protease
  2. Cytochrome P450

Talarozole (Synonyms: R115866)

Cat. No.: HY-14531 Purity: 99.54%
Handling Instructions

Talarozole is a potent inhibitor of both CYP26A1 and CYP26B1, with IC50 of 0.46 nM and 5.1 nM for CYP26B1 and CYP26A1, 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
10 mM * 1 mL in DMSO USD 140 In-stock
2 mg USD 120 In-stock
5 mg USD 168 In-stock
10 mg USD 216 In-stock
50 mg USD 480 In-stock
100 mg USD 780 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of Talarozole:

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

    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.

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

    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 MCE. Usage Cited in: PLoS Genet. 2017 Dec 11;13(12):e1007112.

    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 MCE. Usage Cited in: The University of Texas at Austin. 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).
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Talarozole is a potent inhibitor of both CYP26A1 and CYP26B1, with IC50 of 0.46 nM and 5.1 nM for CYP26B1 and CYP26A1, respectively.

    IC50 & Target

    IC50: 0.46/5.1 nM (CYP26B1/A1)[1]

    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].

    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].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume 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
    10 mM 0.2649 mL 1.3245 mL 2.6489 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [2]

    Talarozole is dissolved in DMSO and stored, and then diluted with appropriate medium before use[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]

    Talarozole is dissolved in DMSO and then diluted with PBS or saline[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
    Molecular Weight

    377.51

    Formula

    C₂₁H₂₃N₅S

    CAS No.

    201410-53-9

    SMILES

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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 36 mg/mL

    Talarozole is dissolved in polyethylene glycol 300 or vehicle control[4].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

    Purity: 99.54%

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    Product Name:
    Talarozole
    Cat. No.:
    HY-14531
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