Acitretin sodium - CAS 925701-88-8
Catalog number: 925701-88-8
Category: Inhibitor
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Molecular Formula:
C21H25NaO3
Molecular Weight:
348.41
COA:
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Targets:
RAR/RXR
Description:
Acitretin sodium is a second-generation, systemic retinoid that has been used in the treatment of psoriasis. It can be considered one of the treatments of choice for pustular and erythrodermic psoriasis. However, the efficacy of acitretin sodium as a monotherapy for plaque psoriasis is less, although it is often used in combination therapy with other systemic psoriasis therapies, especially ultraviolet B or psoralen plus ultraviolet A phototherapy, to increase efficacy. Such combination treatments may potentially minimise toxicity by using lower doses of each of the two agent.
Purity:
>98%
Synonyms:
Ro 10-1670 sodium; Soriatane sodium
MSDS:
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InChIKey:
QTGFSGVSWOBQLB-WMOHYEITSA-N
InChI:
InChI=1S/C21H26O3.Na/c1-14(8-7-9-15(2)12-21(22)23)10-11-19-16(3)13-20(24-6)18(5)17(19)4;/h7-13H,1-6H3,(H,22,23);/b9-7+,11-10+,14-8+,15-12+;
Canonical SMILES:
CC1=CC(=C(C(=C1C=CC(=CC=CC(=CC(=O)O)C)C)C)C)OC.[Na]
1.Effect of sodium lauryl sulfate-induced skin irritation on in vivo percutaneous penetration of four drugs.
Wilhelm KP1, Surber C, Maibach HI. J Invest Dermatol. 1991 Nov;97(5):927-32.
The influence of sodium lauryl sulfate-induced irritant contact dermatitis on in vivo percutaneous penetration was investigated for four 14C-labeled compounds with diverse physicochemical properties: hydrocortisone (HC), indomethacin (IM), ibuprofen (IB), and acitretin (AC). Hairless guinea pigs were pretreated for 24 h with either 0.5% sodium lauryl sulfate (SLS) to induce irritant contact dermatitis or with water (controls). Twenty-four hours after pretreatment, 450 microliters saturated solutions of HC, IM, IB, or AC in isopropylmyristate were applied to the pretreated skin for 24 h. Systemic absorption was determined by urinary and fecal excretion of compounds. Drug concentrations in stratum corneum (obtained by tape cellophane stripping after decontamination of the application site) and in epidermis/dermis (punch biopsy) were also investigated. Systemic absorption of topically applied drugs (as evaluated by urinary and fecal excretion) in SLS-irritated skin was significantly increased for HC (factor 2.
2.Disposition of [14C]acitretin in humans following oral administration.
Rubio F1, Jensen BK, Henderson L, Garland WA, Szuna A, Town C. Drug Metab Dispos. 1994 Mar-Apr;22(2):211-5.
The disposition of the antipsoriatic agent, acitretin, was investigated in six healthy human volunteers who each received a single, oral 50 mg dose of [14C]acitretin (50 microCi). plasma, urine, and feces were collected for 240 hr after administration. Mean values of 20.9 and 62.6% of the administered dose were recovered in the urine and feces, respectively. The terminal elimination half-life of total radioactivity from the plasma was approximately 120 hr. Extraction of pooled plasma samples followed by separation by HPLC and quantitation by liquid scintillation counting indicated that acitretin and its 13-cis-isomer, isoacitretin, were minor fractions of the total drug-related material in the plasma at most time points up to 72-hr postdose. The structures of acitretin, isoacitretin, and two other metabolites--(5E,7E)-8-(4-methoxy,2,3,6-trimethylphenyl)-2,6 -dimethyl-5,7- octadienoic acid (I) and (5E,7E)-8-(4-hydroxy-2,3,6-trimethylphenyl)-2,6-dimethyl-5,7 -octadienoic acid (II)--were confirmed by MS and cochromatography with authentic standards.
3.Influence of the retinoid acitretin on erythrocyte microrheology in vitro.
Górnicki A1. Int J Clin Pharmacol Ther. 2006 Dec;44(12):648-54.
OBJECTIVE: To determine in vitro changes in the microrheology of red blood cells (RBCs) treated with acitretin (Ro 10-1670).
4.Effect of sodium lauryl sulfate-induced skin irritation on in vitro percutaneous absorption of four drugs.
Wilhelm KP1, Surber C, Maibach HI. J Invest Dermatol. 1991 Jun;96(6):963-7.
The influence of irritant contact dermatitis on percutaneous penetration was investigated for four 14C-labeled compounds with diverse physicochemical properties: hydrocortisone (HC), indomethacin (IM), ibuprofen (IB), and acitretin (AC). Hairless guinea pigs were pretreated in vivo for 24 h with either 0.5% sodium lauryl sulfate (SLS) to induce irritant contact dermatitis or with water (controls). Twenty-four hours after pretreatment animals were sacrificed. Percutaneous penetration was then measured using in vitro diffusion cells and the removed (pretreated) skin. The following parameters were determined: cumulative amount of compound penetrated, steady state flux, lag time, and permeability coefficient, skin concentration per unit area, and the relative amount of drug remaining in the skin (as a percentage of the cumulative amount of compound penetrated through the skin). SLS pretreatment resulted in moderate irritant dermatitis in all animals and increased in vivo transepidermal water loss 4.
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CAS 925701-88-8 Acitretin sodium

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