1. Metabolic Enzyme/Protease
  2. Cytochrome P450

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

Cat. No.: HY-14802
Handling Instructions

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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1 mg USD 228 Get quote
5 mg USD 468 Get quote
10 mg USD 780 Get quote
25 mg USD 1800 Get quote
50 mg USD 2880 Get quote

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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].

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.
References
Molecular Weight

377.51

Formula

C₂₁H₂₃N₅S

CAS No.

870093-23-5

SMILES

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

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Talarozole R enantiomer
Cat. No.:
HY-14802
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Talarozole R enantiomer

Cat. No.: HY-14802