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Acitretin Retinoid Receptor agonist

Name: Acitretin
Brand: Selleck Chemicals
SKU: S1368
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S1368

Acitretin (Etretin, RO 10-1670) is a second generation retinoid used for psoriasis.

Chemical Structure

Molecular Weight: 326.43

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.91%

99.91

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Chemical Information, Storage & Stability

Molecular Weight	326.43	Formula	C₂₁H₂₆O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	55079-83-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Etretin, RO 10-1670			Smiles	CC1=CC(=C(C(=C1C=CC(=CC=CC(=CC(=O)O)C)C)C)C)OC

Solubility

In vitro
Batch:

DMSO : 65 mg/mL (199.12 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.600mg/ml (4.90mM)	Taking the 1 mL working solution as an example, add 50 μL of 32 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.130mg/ml (0.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 2.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.

Mechanism of Action

In vitro	Acitretin stimulates ADAM10 promoter activity with an EC(50) of 1.5 mM and leads to an increase of mature ADAM10 protein that results in a two- to three-fold increase of the ratio between alpha- and beta-secretase activity in neuroblastoma cells. ^[1] This compound (5-20 μM) impairs mitochondrial phosphorylation efficiency as demonstrated by the decrease in the state 3 respiration and ATP levels, and by the increase in the lag phase of ADP phosphorylation cycle, without affecting the membrane potential. It induces Ca(2+)-mediated mitochondrial permeability transition (MPT) and decreased the adenine nucleotide translocase (ANT) content. ^[2] The chemical preferentially inhibits the growth of SCL-1 cells in a dose- and time-dependent manner, but not of non-malignant keratinocyte HaCaT cells. It increases the levels of CD95 (Fas), CD95-ligand and Fas-associated death domain. It is able to induce apoptosis in skin cancer cells possibly via death receptor CD95 apoptosis pathway without affecting the viability of normal keratinocyte. ^[3]
In vivo	Acitretin undergoes alpha-oxidation, chain shortening O-demethylation, and glucuronidation in the perfused rat liver. ^[4] This compound rapidly appears in liver and muscle of rats, where it undergoes redistribution into skin and adipose tissue. ^[5]
References	[1] https://pubmed.ncbi.nlm.nih.gov/19144697/ [2] https://pubmed.ncbi.nlm.nih.gov/23384448/ [3] https://pubmed.ncbi.nlm.nih.gov/18624760/ [4] https://pubmed.ncbi.nlm.nih.gov/1492415/ [5] https://pubmed.ncbi.nlm.nih.gov/8149885/

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04841187	Completed	Psoriasis	Assistance Publique - Hôpitaux de Paris\|Société de Dermatologie Française	September 6 2021	--
NCT04245319	Unknown status	Hyperlipidemias\|Xerosis\|Depression\|Liver Diseases	Cairo University	January 1 2020	Not Applicable
NCT05203354	Completed	Psoriasis	Mahmoud Ahmed Ali Ahmed\|Aswan University Hospital	September 1 2018	Phase 4
NCT01039142	Completed	Psoriasis	Post Graduate Institute of Medical Education and Research Chandigarh\|PIMERIndia	March 2008	Phase 4
NCT00488384	Withdrawn	Carcinoma Squamous Cell	Günther Hofbauer\|University of Zurich	June 2007	Phase 4
NCT00156247	Completed	Psoriasis	University of Medicine and Dentistry of New Jersey\|Connetics Corp.\|Rutgers The State University of New Jersey	September 2005	Phase 2

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