2. Metabolic Enzyme/Protease
  3. Cytochrome P450
  4. 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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Based on 1 publication(s) in Google Scholar

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Talarozole (R enantiomer) Related Antibodies

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

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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)[C@H](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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
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Purity & Documentation
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Complete Stock Solution Preparation Table

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
100 mM 0.0265 mL 0.1324 mL 0.2649 mL 0.6622 mL
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Talarozole (R enantiomer) Related Classifications

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  • 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:

Talarozole (R enantiomer)870093-23-5(R)-TalarozoleCytochrome P450CYPsInhibitorinhibitorinhibit

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