Tazarotene is a member of the acetylenic class of retinoids which binds at retinoid acid receptors (RAR) -β and -γ.Tazarotene is a retinoic acid receptor-specific retinoid with demonstrated efficacy in the topical treatment of psoriasis.Tazarotene exerts anti-inflammatory and immune-modulating activities toward both infective agents and damaged keratinocytes.Tazarotene down-regulates markers of keratinocyte differentiation, keratinocyte proliferation, and inflammation.It is also up-regulates three novel genes TIG-1 (tazarotene-induced gene-1), TIG-2, and TIG-3, which may mediate an antiproliferative effect.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO >10 mg/mL|
Tazarotene as alternative topical treatment for onychomycosis.
Campione E, et al. Drug Des Devel Ther. 2015 Feb 16;9:879-86. PMID: 25733808.
Tazarotene induces apoptosis in human basal cell carcinoma via activation of caspase-8/t-Bid and the reactive oxygen species-dependent mitochondrial pathway.
Wu CS, et al. DNA Cell Biol. 2014 Oct;33(10):652-66. PMID: 24927175.
Molecular mechanisms of tazarotene action in psoriasis.
Duvic M, et al. J Am Acad Dermatol. 1997 Aug;37(2 Pt 3):S18-24. PMID: 9270552.
|Related RAR/RXR Products|
HX 531 is a potent antagonist of retinoid X receptors (IC50 = 18 nM).
MM11253 (SR11253) is a high-affinity RARγ-selective retinoid acid (RA) receptor antagonist (IC50 = 44 nM against ATRA for binding RARγ; IC50 =1 μM in case of RARα, RARβ, RXRα).
CD437 is a retinoic acid receptor (RAR)γ-selective agonist, γ-selective retinoid; potent inducer of apoptosis.
Bexarotene is a retinoid specifically selective for retinoid X receptors, used as an oral antineoplastic agent in the treatment of cutaneous T-cell lymphoma.
Fenretinide (4-HPR) is a synthetic retinoid deriverative. Fenretinide is shown to exhibit binding to the retinoic acid receptors (RAR) at concentrations necessary to induce cell death.
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