Tazarotene 是一种选择性视黄酸受体激动剂,用于研究寻常痤疮和斑块状银屑病。
产品描述
Tazarotene is a synthetic, topical retinoid. Tazarotene induces the expression of tazarotene-induced gene 3 (TIG3), a tumor suppressor gene. In psoriasis, tazarotene normalizes abnormal keratinocyte differentiation and reduces their hyperproliferation.
体外活性
Tazarotene causes ERK activation, RB tumor suppressor protein hypophosphorylation, G0 arrest, and myeloid differentiation in HL-60 human myeloblastic leukemia cells. Tazarotene could propel either early or late portions of the period leading to differentiation and G0 arrest and is interchangeable with an RARalpha-selective ligand. [1] Tazarotene therapy regulates gene transcription via interaction with specific nuclear retinoic acid receptors (RARs), thereby modulating the three key pathogenic factors in psoriasis. [2] Tazarotene inhibits the proliferation of fibroblasts and synthesis of DNA and collagen. [3] Tazarotene down-regulates markers of keratinocyte differentiation, keratinocyte proliferation, and inflammation. Tazarotene also up-regulates three novel genes TIG-1 (tazarotene-induced gene-1), TIG-2, and TIG-3, which may mediate an antiproliferative effect. [4] Tazarotene causes growth suppression in retinoid-responsive breast cancer cell lines by up-regulating TIG3. [5]
体内活性
Tazarotene treatment reduces the number and size of microscopic basal cell carcinomas (BCCs) in UV-treated Ptch1+/? mice. Tazarotene treatment reduces the number and size of microscopic basal cell carcinomas (BCCs) in ionizing radiation-treated Ptch1+/? mice. [5]
Cas No.
118292-40-3
分子式
C21H21NO2S
分子量
351.46
别名
Tazorac;他扎罗汀;Zorac;AGN 190168
储存和溶解度
DMSO:35.2 mg/mL (100 mM)
Ethanol:17.6 mg/mL (50 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years