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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) Chemical Structure
CAS No. : 870093-23-5
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是否有货 |
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| 100 mg |
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| 250 mg |
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| 500 mg |
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* Please select Quantity before adding items.
| 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].
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 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 |
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| 参考文献 |
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[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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