Tazarotene

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Chemical Structure| 118292-40-3 同义名 : AGN 190168
CAS号 : 118292-40-3
货号 : A357060
分子式 : C21H21NO2S
纯度 : 97%
分子量 : 351.462
MDL号 : MFCD00867628
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(142.26 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Retinoids bind to retinoic acid receptors (RARs) and retinoid X receptors (RXRs) to regulate the expression of genes involved in cell growth and differentiation. Tazarotene is an acetylenic retinoid that can be metabolized by esterase to its active form, tazarotene acid, that acts as a RARb/g specific retinoid. Tazarotene at the dose of 1 μM decreased the proliferation of primary human skin fibroblasts 4 days after the treatment and inhibited the growth rate at day 6. Tazarotene form 0.001 – 10 μM also suppressed BdrU incorporation at a dose-dependent manner and the significant inhibition was found at the doses of 0.1 μM and above. The maximal inhibition of tazarotene on BrdU incorporation was observed at 1 μM, which was 22% that of the control cells, and the IC50 value was 60 nM[5]. Treatment of reconstructed human epidermis tissues with tazarotene (0.1% cream) for 3 days resulted in a loss of keratohyalin granules in the stratum granulosum compared to vehicle-treated cultures. Also, in tazarotene-treated tissues, the kerain 10 expression in the stratum spinosum was lower than that in untreated controls, while the expression of kerain 19 was significantly induced in all viable cell layers. In Rhino mouse model, daily administration of tazarotene (0.1% cream, 7 days) completed (100%) reduced the utricle diameter compared to water- or vehicle-treated animals[6].
作用机制 Tazarotene is a prodrug that can be metabolized into its active free-acid form, tazarotene acid. As a receptor-selective retinoid, it incorporates the double bonds of the retinoic acid polyene chain in two ring structures and a linear triple bond system[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.85mL

0.57mL

0.28mL

14.23mL

2.85mL

1.42mL

28.45mL

5.69mL

2.85mL

参考文献

[1]Talpur R, Cox K, et al. Efficacy and safety of topical tazarotene: a review. Expert Opin Drug Metab Toxicol. 2009 Feb;5(2):195-210.

[2]Nagpal S, Thacher SM, et al. Negative regulation of two hyperproliferative keratinocyte differentiation markers by a retinoic acid receptor-specific retinoid: insight into the mechanism of retinoid action in psoriasis. Cell Growth Differ. 1996 Dec;7(12):1783-91.

[3]Tazarotene, a Retinoic Acid Receptor (RAR) Agonist, Protects Photoreceptor in a Blue Light–Induced Retinal Degeneratio Model

[4]Al Haj Zen A, Nawrot DA, et al. The Retinoid Agonist Tazarotene Promotes Angiogenesis and Wound Healing. Mol Ther. 2016 Oct;24(10):1745-1759.

[5]Ogawa A, Maeguchi M, Uchida Y, Yoshioka T, Kawashima M, Muraki T. Effect of tazarotene, an acetylenic retinoid, on human dermal fibroblast. Jpn J Pharmacol. 1998 Mar;76(3):317-9.

[6]Hsia E, Johnston MJ, Houlden RJ, Chern WH, Hofland HE. Effects of topically applied acitretin in reconstructed human epidermis and the rhino mouse. J Invest Dermatol. 2008 Jan;128(1):125-30.

[7]Chandraratna RA. Tazarotene--first of a new generation of receptor-selective retinoids. Br J Dermatol. 1996 Oct;135 Suppl 49:18-25.