A retinoid prodrug of tazarotenic acid; inhibits proliferation and collagen synthesis by human dermal fibroblasts (1 μM); downregulates markers of keratinocyte differentiation

Tazarotene – 5 mg

Brand:
Cayman
CAS:
118292-40-3
Storage:
-20
UN-No:
Non-Hazardous - /

Tazarotene is a retinoid prodrug of tazarotenic acid (Item No. 21367).{33614} It is metabolized by esterases in vivo to its active free acid form. Tazarotene (1 μM) inhibits proliferation of and collagen synthesis by human dermal fibroblasts in vitro.{41677} It also downregulates markers of keratinocyte differentiation, keratinocyte proliferation, and inflammation and upregulates tazarotene-induced gene 1 (TIG1) and TIG2 in patient-derived psoriatic lesion samples following topical administration.{41678} Tazarotene (0.1% per day, topical) induces complete reduction in skin utricle diameter in the Rhino mouse, which is a model used to test retinoid activity because its skin contains keratinized pilosebaceous structures.{41679} It also decreases basal cell carcinoma number and size in a Ptch1+/- mouse model of ultraviolet- or ionizing radiation-induced skin cancer when administered topically at a dose of 0.1% per day.{41680} Formulations containing tazarotene have been used in the treatment of psoriasis, acne, and sun-damaged skin.  

 

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Description

A retinoid prodrug of tazarotenic acid; inhibits proliferation and collagen synthesis by human dermal fibroblasts (1 μM); downregulates markers of keratinocyte differentiation, keratinocyte proliferation, and inflammation and upregulates TIG1 and TIG2 in human-derived psoriatic lesions following topical administration; induces complete reduction of skin utricle diameter in the Rhino mouse (0.1% per day, topical); decreases basal cell carcinoma number and size in a Ptch1+/- mouse model of ultraviolet- or ionizing radiation-induced skin cancer when (0.1% per day, topical)

Formal name: 6-[2-(3,4-dihydro-4,4-dimethyl-2H-1-benzothiopyran-6-yl)ethynyl]-3-pyridinecarboxylic acid, ethyl ester

Synonyms:  AGN 190168

Molecular weight: 351.5

CAS: 118292-40-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Immunology & Inflammation|Autoimmunity

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