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

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

Talarozole R enantiomer是一个强的，有选择性的细胞色素P450，CYP26的抑制剂。

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

Talarozole (R enantiomer) Chemical Structure

CAS No. : 870093-23-5

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生物活性

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].

分子量

377.51

Formula

C21H23N5S
CAS 号

870093-23-5
中文名称

(R)-他拉罗唑
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
溶解性数据
In Vitro: 

DMSO : ≥ 51 mg/mL (135.10 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 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

参考文献

  • [1]. Pavez Loriè E, Cools M, Borgers M, Topical treatment with CYP26 inhibitor talarozole (R115866) dose dependently alters the expression of retinoid-regulated genes in normal human epidermis. Br J Dermatol. 2009 Jan;160(1):26-36

    [2]. Geria AN, Scheinfeld NS. Talarozole, a selective inhibitor of P450-mediated all-trans retinoic acid for the treatment of psoriasis and acne. Curr Opin Investig Drugs. 2008 Nov;9(11):1228-37.

    [3]. Baert B, De Spiegeleer B. Local skin pharmacokinetics of talarozole, a new retinoic acid metabolism-blocking agent. Skin Pharmacol Physiol. 2011;24(3):151-9.

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