Tazarotene (Synonyms: AGN 190168)

Name: Tazarotene
Brand: MedChemExpress
SKU: HY-15388
Rating: 5.0 (2 reviews)

Cat. No.: HY-15388 Purity: 99.83%: FAQs
Data Sheet SDS COA Handling Instructions

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Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris. Tazarotene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

For research use only. We do not sell to patients.

Tazarotene Chemical Structure

CAS No. : 118292-40-3

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 42	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 224	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 356	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Tazarotene:

2 Publications Citing Use of MCE Tazarotene

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RXRα RXRβ RXRγ

Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
COS-7	EC₅₀	0.8 nM Compound: tazarotene	Activity at human RARbeta ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay Activity at human RARbeta ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay	[PMID: 19058965]
COS-7	EC₅₀	40 nM Compound: tazarotene	Activity at human RARgamma ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay Activity at human RARgamma ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay	[PMID: 19058965]
COS-7	EC₅₀	63 nM Compound: tazarotene	Activity at human RARalpha ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay Activity at human RARalpha ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay	[PMID: 19058965]

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^[1]. 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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[3].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^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

351.46

Formula

C₂₁H₂₁NO₂S

CAS No.

118292-40-3

Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (142.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.83%

Select Batch:

Data Sheet (275 KB) SDS (418 KB)

COA (249 KB) LCMS (300 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.8453 mL	14.2264 mL	28.4527 mL	71.1319 mL
	5 mM	0.5691 mL	2.8453 mL	5.6905 mL	14.2264 mL
	10 mM	0.2845 mL	1.4226 mL	2.8453 mL	7.1132 mL
	15 mM	0.1897 mL	0.9484 mL	1.8968 mL	4.7421 mL
	20 mM	0.1423 mL	0.7113 mL	1.4226 mL	3.5566 mL
	25 mM	0.1138 mL	0.5691 mL	1.1381 mL	2.8453 mL
	30 mM	0.0948 mL	0.4742 mL	0.9484 mL	2.3711 mL
	40 mM	0.0711 mL	0.3557 mL	0.7113 mL	1.7783 mL
	50 mM	0.0569 mL	0.2845 mL	0.5691 mL	1.4226 mL
	60 mM	0.0474 mL	0.2371 mL	0.4742 mL	1.1855 mL
	80 mM	0.0356 mL	0.1778 mL	0.3557 mL	0.8891 mL
	100 mM	0.0285 mL	0.1423 mL	0.2845 mL	0.7113 mL

Tazarotene Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tazarotene118292-40-3AGN 190168AGN190168AGN-190168RAR/RXRAutophagyRetinoic acid receptorsRetinoid X receptorsInhibitorinhibitorinhibit

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Tazarotene (Synonyms: AGN 190168)

Customer Review

Other Forms of Tazarotene:

Tazarotene Related Antibodies

2 Publications Citing Use of MCE Tazarotene

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All RAR/RXR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Tazarotene Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Tazarotene Related Classifications

Keywords:

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Customer Review

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