1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. Talarozole (R enantiomer)

Talarozole (R enantiomer) (Synonyms: (R)-Talarozole)

Cat. No.: HY-14802
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Talarozole R enantiomer is a potent and selective inhibitor of cytochrome P450 26-mediated breakdown of endogenous all-trans retinoic acid for the treatment of psoriasis and acne.

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

Talarozole (R enantiomer) Chemical Structure

Talarozole (R enantiomer) Chemical Structure

CAS No. : 870093-23-5

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Description

Talarozole R enantiomer is a potent and selective inhibitor of cytochrome P450 26-mediated breakdown of endogenous all-trans retinoic acid for the treatment of psoriasis and acne. Target: CYP26 in vitro: Talarozole R enantiomer treatment increased the mRNA expression of CRABP2, KRT4, CYP26A1 and CYP26B1 dose dependently, and decreased theexpression of KRT2 and IL-1alpha compared with vehicle-treated skin. No mRNA change in retinol-metabolizing enzymes was obtained. There was no induction of epidermal thickness or overt skin inflammation in talarozole-treated skin. Immunofluorescence analysis confirmed an upregulation of KRT4 protein, but no upregulation of CYP26A1 and CYP26B1 expression was detected [1] [2]. in vivo: Talarozole R enantiomer slightly diffused into the skin only when dissolved in propylene glycol, isopropyl myristate or ethanol. Although only 0.1% of the dose applied was found in the skin itself after 12-24 h, this was sufficient to achieve local concentrations well above the half-maximal inhibitory concentration value for talarozole. The distribution of talarozole within the skin was investigated: 80% was located in the epidermis, while the remaining 20% was found in the dermis [3].

Molecular Weight

377.51

Formula

C₂₁H₂₃N₅S

CAS No.
SMILES

CCC(CC)[[email protected]](C1=CC=C(NC2=NC3=CC=CC=C3S2)C=C1)N4N=CN=C4

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : ≥ 51 mg/mL (135.10 mM)

*"≥" means soluble, but saturation unknown.

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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
10 mM 0.2649 mL 1.3245 mL 2.6489 mL
*Please refer to the solubility information to select the appropriate solvent.
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Keywords:

Talarozole (R enantiomer)(R)-TalarozoleCytochrome P450CYPsInhibitorinhibitorinhibit

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Talarozole (R enantiomer)
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