| 產品描述： | Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris |
| 靶點： |
RAR/RXR;Autophagy;RetinoidReceptor;Autophagy |
| 體外研究： |
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. |
| 體內研究： |
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. |
| 參考文獻： |
1. Talpur R, et al. Efficacy and safety of topical tazarotene: a review. Expert Opin Drug Metab Toxicol. 2009 Feb;5(2):195-210.
2. Nagpal S, et al. Negative regulation of two hyperproliferative keratinocyte differentiation markers by a retinoic acidreceptor-specific retinoid: insight into the mechanism of retinoid action in psoriasis. Cell Growth Differ. 1996 Dec;7(12):1783-91.
3. Tang-Liu DD, et al. Clinical pharmacokinetics and drug metabolism of tazarotene: a novel topical treatment for acne and psoriasis. Clin Pharmacokinet. 1999 Oct;37(4):273-87. |
| 溶解性： |
soluble in DMSO |
| 保存條件： |
2-8℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.845 ml |
14.226 ml |
28.453 ml |
| 5 mM |
0.569 ml |
2.845 ml |
5.691 ml |
| 10 mM |
0.285 ml |
1.423 ml |
2.845 ml |
| 50 mM |
0.057 ml |
0.285 ml |
0.569 ml |
|
| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京