产品
编 号:F058655
分子式:C21H21NO2S
分子量:351.46
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10mM*1mL in DMSO
询价
询价
5mg
250
In-stock
10mg
399
In-stock
50mg
1280
In-stock
100mg
1960
In-stock
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产品详情
生物活性:
Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris. Tazarotene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

体内研究:
Topical gel application provides direct delivery of Tazarotene (AGN 190168) into the skin. At 10 hours after a topical application of 0.1% Tazarotene (AGN 190168) gel to the skin of healthy individuals and patients with psoriasis, approximately 4 to 6% of the dose resides in the stratum corneum and 2% of the dose distributed to the viable epidermis and dermis. Tazarotene (AGN 190168) is designed to undergo rapid and complete metabolism to its active metabolite tazarotenic acid. Tazarotenic acid has a short systemic residence time and limited tissue distribution in animals.When topically applied, Tazarotene (AGN 190168) blocks the induction of ornithine decarboxylase (ODC) activity by the tumour promoter 12-O-tetradecanoylphorbol 13-acetate (TPA) in the epidermis of the hairless mouse.

体外研究:
Tazarotene (AGN 190168), in both gel and cream formulations, has been used both as monotherapy and as an adjuvant therapy. For psoriasis it has been combined with steroids, calcipotriene and phototherapy, and for acne, with antibiotics. Tazarotene (AGN 190168) has been shown to upregulate the tumor suppressor, Tazarotene (AGN 190168) induced gene 3, which is overexpressed in psoriasis and skin cancer. In human epidermal cell cultures, Tazarotene (AGN 190168) suppresses the gene expression of 2 marker proteins, MRP-8 (calgranulin A) and SKALP (skin derived anti-leukoproteinase), highly elevated in psoriatic epidermis.
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