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Acitretin Retinoid Receptor agonist

Cat.No.S1368

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

Batch: Purity: 99.91%
99.91

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

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In vivo
Batch:

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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.
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Chemical Information, Storage & Stability

Molecular Weight 326.43 Formula

C21H26O3

Storage (From the date of receipt)
CAS No. 55079-83-9 Download SDF Storage of Stock Solutions

Synonyms Etretin, RO 10-1670 SMILES CC1=CC(=C(C(=C1C=CC(=CC=CC(=CC(=O)O)C)C)C)C)OC

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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. 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. 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.
In vivo
Acitretin undergoes alpha-oxidation, chain shortening O-demethylation, and glucuronidation in the perfused rat liver. This compound rapidly appears in liver and muscle of rats, where it undergoes redistribution into skin and adipose tissue.
References
  • [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 2022-11-25)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04537689 RECRUITING
Plaque Psoriasis
Singapore General Hospital
2020-12-10 PHASE4
NCT04239859 NOT_YET_RECRUITING
Plaque Psoriasis
Singapore General Hospital
2024-01 PHASE4
NCT06998875 RECRUITING
Primary Cutaneous Amyloidosis
Army Medical University, China
2025-03-01 PHASE4
NCT07708480 COMPLETED
Hidradenitis Suppurativa
Hayat Abad Medical Complex, Peshawar
2024-12-22 PHASE4
NCT06739551 NOT_YET_RECRUITING
Lichen Planus
Sheikh Zayed Medical College
2024-12-10 PHASE2
NCT05184348 COMPLETED
Psoriasis Vulgaris
South Valley University
2021-09-01 PHASE1

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