research use only

Tazarotene Retinoid Receptor agonist

Cat.No.S1569

Tazarotene (AGN190168) is a retinoid prodrug of tazarotenic acid, which is a RAR agonist, used to treat psoriasis, acne, and sun damaged skin.
Tazarotene  Retinoid Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 351.46

Jump to

Quality Control

Batch: Purity: 99.98%
99.98

Solubility

In vitro
Batch:

DMSO : 10 mg/mL (28.45 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg
g
μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
+
%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 351.46 Formula

C21H21NO2S

Storage (From the date of receipt)
CAS No. 118292-40-3 Download SDF Storage of Stock Solutions

Synonyms AGN190168 Smiles CCOC(=O)C1=CN=C(C=C1)C#CC2=CC3=C(C=C2)SCCC3(C)C

Mechanism of Action

Targets/IC50/Ki
RAR
In vitro
Tazarotene causes ERK activation, RB tumor suppressor protein hypophosphorylation, G0 arrest, and myeloid differentiation in HL-60 human myeloblastic leukemia cells. This compound could propel either early or late portions of the period leading to differentiation and G0 arrest and is interchangeable with an RARalpha-selective ligand. It regulates gene transcription via interaction with specific nuclear retinoic acid receptors (RARs), thereby modulating the three key pathogenic factors in psoriasis. This chemical inhibits the proliferation of fibroblasts and synthesis of DNA and collagen. It down-regulates markers of keratinocyte differentiation, keratinocyte proliferation, and inflammation. This agent also up-regulates three novel genes TIG-1 (tazarotene-induced gene-1), TIG-2, and TIG-3, which may mediate an antiproliferative effect. It causes growth suppression in retinoid-responsive breast cancer cell lines by up-regulating TIG3.
In vivo
Tazarotene treatment reduces the number and size of microscopic basal cell carcinomas (BCCs) in UV-treated Ptch1+/− mice. This compound also reduces the number and size of microscopic basal cell carcinomas (BCCs) in ionizing radiation-treated Ptch1+/− mice.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/9270552/
  • [5] https://pubmed.ncbi.nlm.nih.gov/15231643/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06015152 Completed
Scalp Psoriasis
Jinnah Postgraduate Medical Centre
August 1 2022 Not Applicable
NCT03988439 Recruiting
Psoriasis
Bausch Health Americas Inc.
March 24 2021 Phase 4
NCT02620813 Completed
Acne Vulgaris
University of California Davis
October 2015 Early Phase 1

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.