| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Tazarotene (AGN 190168, AGN190168,Tazarotene, Fabior, Zorac; AGN-190168), a third-generation prescription topical retinoid, is a prodrug of tazarotenic acid with selective affinity for RARβ and RARγ. Tazarotene has to be converted to its active form, the cognate carboxylic acid of tazarotene, by rapid deesterification in animals and humans.
| ln Vitro |
Tazarotene (AGN 190168) can be used as an adjuvant or as a monotherapy. It comes in gel and cream formulations. It is used in conjunction with steroids, calcipotriene, and phototherapy for psoriasis, and antibiotics in combination with it for acne. The tumor suppressor tazarotene (AGN 190168)-induced gene 3, which is overexpressed in psoriasis and skin cancer, has been demonstrated to be upregulated by tazarotene (AGN 190168) [1]. Tazorotene (AGN 190168) decreases the expression of two marker proteins associated in psoriasis, MRP-8 (calgranulin A) and SKALP (skin-derived antialbumin A), in human epidermal cell cultures. increased epidermal height [2].
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| ln Vivo |
Tazarotene (AGN 190168) is applied topically as a gel, straight into the skin. Approximately 4% to 6% of the 0.1% tazarotene (AGN 190168) gel was maintained in the stratum corneum and 2% was disseminated to the epidermis and dermis in vivo following topical application of the gel to the skin of both healthy individuals and psoriasis sufferers for 10 hours. It is intended for tazarotene (AGN 190168) to be fully and quickly converted into tazarotenic acid, which is its active metabolite. In animals, tazarotene acid has a brief duration of systemic residence and a restricted tissue distribution [3]. When administered topically, tazarotene (AGN 190168) inhibits the activity of ornithine decarboxylase (ODC) (TPA) generated by the tumor promoter 12-O-tetradecanoylphorbol 13-acetate (13-acetate) in the epidermis of hairless mice [3].
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| References |
[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. |
| Molecular Formula |
C21H21NO2S
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|---|---|
| Molecular Weight |
351.464
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| Exact Mass |
351.1293
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| CAS # |
118292-40-3
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| Related CAS # |
Tazarotene-d8
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| SMILES |
S1C2C([H])=C([H])C(C#CC3C([H])=C([H])C(C(=O)OC([H])([H])C([H])([H])[H])=C([H])N=3)=C([H])C=2C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])C1([H])[H]
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| Synonyms |
AGN 190168, Tazarotene, Fabior, Zorac AGN190168, AGN-190168
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~142.26 mM)
: 0.1 mg/mL (~0.28 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8453 mL | 14.2264 mL | 28.4527 mL | |
| 5 mM | 0.5691 mL | 2.8453 mL | 5.6905 mL | |
| 10 mM | 0.2845 mL | 1.4226 mL | 2.8453 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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