Acitretin sodium - CAS 925701-88-8
Not Intended for Therapeutic Use. For research use only.
Category:
Inhibitor
Product Name:
Acitretin sodium
Catalog Number:
925701-88-8
Synonyms:
Ro 10-1670 sodium; Soriatane sodium
CAS Number:
925701-88-8
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.
Molecular Weight:
348.41
Molecular Formula:
C21H25NaO3
COA:
Inquire
MSDS:
Inquire
Targets:
RAR/RXR
Chemical Structure
CAS 925701-88-8 Acitretin sodium

Related RAR/RXR Products


CAS 4759-48-2 Isotretinoin

Isotretinoin
(CAS: 4759-48-2)

Isotretinoin, also known as 13-cis retinoic acid and first marketed as Accutane by Hoffmann-La Roche, is an oral pharmaceutical drug primarily used to treat cys...

CAS 118292-40-3 Tazarotene

Tazarotene
(CAS: 118292-40-3)

Tazarotene could propel either early or late portions of the period leading to differentiation and G0 arrest and is interchangeable with an RARalpha-selective l...

CAS 55079-83-9 Acitretin

Acitretin
(CAS: 55079-83-9)

Acitretin is a second generation retinoid used for psoriasis.

CAS 153559-49-0 Bexarotene

Bexarotene
(CAS: 153559-49-0)

Bexarotene is a retinoid specifically selective for retinoid X receptors, used as an oral antineoplastic agent in the treatment of cutaneous T-cell lymphoma.

CAS 229961-45-9 AGN 194310

AGN 194310
(CAS: 229961-45-9)

A high affinity pan-RAR antagonist (AGN194310, K(d) for binding to RARs = 2-5 nM) inhibited colony formation (by 50%) by all three lines at 16-34 nM, and led to...

NRX-204647
(CAS: 1351452-80-6)

NRX-204647 is a Retinoic acid receptor gamma-selective inverse agonist.

CAS 958295-17-5 AGN 196996

AGN 196996
(CAS: 958295-17-5)

AGN 196996 is a potent and selective antagonist of RARα. It has been reported to selectively bind to RARs (retinoic acid receptors) for RARα, RARβ and RARγ. It...

CAS 106685-40-9 Adapalene

Adapalene
(CAS: 106685-40-9)

Adapalene is more active than indomethacin, betamethasone valerate, tretinoin, isotretinoin or etretinate in inhibiting lipoxygease activity, but it has little ...

CAS 911110-93-5 Adapalene sodium salt

Adapalene sodium salt
(CAS: 911110-93-5)

Adapalene sodium salt, a synthetic retinoid, is a Retinoic acid receptor agonist (RAR). It is a third-generation topical retinoid primarily used in the treatmen...

CAS 71441-28-6 TTNPB

TTNPB
(CAS: 71441-28-6)

TTNPB potently and selectively activates retinoic acid receptors (EC50s = 21, 4, and 2.4 nM for RARα, RARβ, and RARγ, respectively). And it does not act on reti...

CAS 65646-68-6 Fenretinide

Fenretinide
(CAS: 65646-68-6)

Fenretinide is an orally-active synthetic phenylretinamide analogue of retinol (vitamin A) with potential antineoplastic and chemopreventive activities. Fenreti...

CAS 410528-02-8 Palovarotene

Palovarotene
(CAS: 410528-02-8)

Palovarotene is a selective retinoic acid receptor gamma(RAR-γ) agonist for the treatment of emphysema. In small animal studies, palovarotene was claimed to rev...

HX-603
(CAS: 259228-72-3)

HX-603 is a RXR agonist.

CAS 102121-60-8 AM580

AM580
(CAS: 102121-60-8)

AM580 is a stable retinobenzoic derivative originally synthesized as a RARα agonist (EC50 values are 0.3, 8.6 and 13 nM for RARα, RARβ and RARγ respectively).

LY2955303
(CAS: 1433497-19-8)

LY2955303 is a selective Retinoic acid receptor gamma (RAR-γ) antagonist with Ki of 1.09 nM; (RAR-α Ki > 1700 nM; RAR-β Ki > 2980 nM). LY2955303 showed good pha...

CAS 859498-05-8 AGN 205728

AGN 205728
(CAS: 859498-05-8)

AGN 205728 is a potent and selective RARγ antagonist and has no inhibiton on RARα and RARβ.

CAS 107430-66-0 CD1530

CD1530
(CAS: 107430-66-0)

CD1530 is a potent and selective retinoic acid receptor(RAR) agonist with Ki values of 150, 1500 and 2750 nM for RARγ, RARβ and RARα receptors respectively. It ...

CAS 94497-51-5 Tamibarotene

Tamibarotene
(CAS: 94497-51-5)

Tamibarotene is a retinoic acid receptor α (RARα) agonist that induces differentiation and apoptosis of HL-60 cells in vitro. It exhibits antiproliferative effe...

UAB30
(CAS: 205252-59-1)

UAB30 is a low-toxicity retinoid X receptor-selective agonist selective for the binding and activation of RXR’s over RAR' s. UAB30 is highly effective in the pr...

CAS 925701-88-8 Acitretin sodium

Acitretin sodium
(CAS: 925701-88-8)

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 choic...

Reference Reading


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.