Tazarotene

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

他扎罗汀是他扎罗汀酸的类视黄醇前药，他扎罗汀酸是一种 RAR 激动剂，用于治疗牛皮癣、痤疮和晒伤皮肤。

Tazarotene is a retinoid prodrug of tazarotenic acid, which is a RAR agonist, used to treat psoriasis, acne, and sun damaged skin.(In Vitro):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. (In Vivo):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.

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.

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.

AGN 190168

Metabolic Enzyme/Protease

Retinoid Receptor

RAR

Inflammation/Immunology

——

118292-40-3

351.46

C21H21NO2S

>98% (HPLC)

Ethanol: 10 mg/mL (28.45 mM); DMSO: 10 mg/mL (28.45 mM)

O=C(OCC)C1=CN=C(C#CC2=CC(C(C)(C)CCS3)=C3C=C2)C=C1

ethyl 6-((4,4-dimethylthiochroman-6-yl)ethynyl)nicotinate

(-20℃)

With Ice Pack

≥ 2 years