Adapalene - CAS 106685-40-9
Not Intended for Therapeutic Use. For research use only.
Category:
Inhibitor
Product Name:
Adapalene
Catalog Number:
106685-40-9
Synonyms:
CD-271
CAS Number:
106685-40-9
Description:
Adapalene is more active than indomethacin, betamethasone valerate, tretinoin, isotretinoin or etretinate in inhibiting lipoxygease activity, but it has little activity against cyclo-oxygenase.
Molecular Weight:
412.52
Molecular Formula:
C28H28O3
COA:
Inquire
MSDS:
Inquire
Targets:
RAR/RXR
Chemical Structure
CAS 106685-40-9 Adapalene

Related RAR/RXR Products


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 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 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 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...

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...

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

HX-603 is a RXR agonist.

CAS 55079-83-9 Acitretin

Acitretin
(CAS: 55079-83-9)

Acitretin is a second generation retinoid used for psoriasis.

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...

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...

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...

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 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 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 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).

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...

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 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.

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 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...

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

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

Reference Reading


1.Recent advances in the use of adapalene 0.1%/benzoyl peroxide 2.5% to treat patients with moderate to severe acne.
Leyden J1. J Dermatolog Treat. 2016 Mar;27 Suppl 1:S4-S13. doi: 10.3109/09546634.2016.1145338.
The central role of inflammation in acne is now more clearly understood. Adapalene, a third-generation topical retinoid, down-regulates toll-like receptor 2 expression and inhibits activator protein-1 activity. In a fixed-dose combination, adapalene and benzoyl peroxide (BPO) act synergistically on inflammatory patterns through regulation of innate immunity. In addition to reducing inflammatory and non-inflammatory lesions, adapalene/BPO helps prevent lesion and microcomedone formation. The combination of a topical retinoid and antimicrobial agent remains the preferred approach for almost all patients with acne. In cases of more severe disease, there is a clinical benefit in combining adapalene/BPO with an oral antibiotic for 12 weeks. Most recently, adapalene/BPO plus doxycycline 200 mg was found to be highly effective when compared with isotretinoin in the treatment of patients with severe acne with nodules. Long-term maintenance therapy is needed for most patients.
2.Customized Single-agent Therapy Management of Severe Inflammatory Acne: A Randomized, Double-blind, Parallel-group, Controlled Study of a New Treatment--Adapalene 0.3%-Benzoyl Peroxide 2.5% Gel.
Weiss J, Stein Gold L, Leoni M, Rueda MJ, Liu H, Tanghetti E. J Drugs Dermatol. 2015 Dec;14(12):1427-35.
BACKGROUND: More effective therapies are needed in the specific treatment of severe inflammatory acne vulgaris.
3.Accelerated Onset of Action and Increased Tolerability in Treating Acne With a Fixed-Dose Combination Gel.
Friedman A, Waite K, Brandt S, Meckfessel MH. J Drugs Dermatol. 2016 Feb 1;15(2):231-6.
Nonadherence to topical acne therapies is a major contributing factor to poor treatment outcomes. Multiple contributing factors have been identified, including a lack of perceived efficacy and fear of side effects. A fixed-dose combination gel of adapalene/benzoyl peroxide gel, 0.1%/2.5% (A-BPO) is an efficacious and safe treatment for a range of acne severities in patients as young as 9 years old. A meta-analysis of 14 clinical studies involving A-BPO was conducted to assess the 4 week efficacy and overall tolerability of this treatment. Over 2,300 subjects were included in the analysis. Mean total, inflammatory, and non-inflammatory lesion counts decreased at 4 weeks by 40.8%, 46.2%, and 37.5%, respectively. Worst post-baseline tolerability scores for stinging/burning, dryness, scaling, and erythema were none or mild for a majority of subjects. The result of this meta-analysis add to the body of literature supporting the use of A-BPO in a variety of acne patients and shows that A-BPO provides meaningful clinical results within 4 weeks and will be well-tolerated for a majority of patients.
4.Moderate and Severe Inflammatory Acne Vulgaris Effectively Treated with Single-Agent Therapy by a New Fixed-Dose Combination Adapalene 0.3 %/Benzoyl Peroxide 2.5 % Gel: A Randomized, Double-Blind, Parallel-Group, Controlled Study.
Stein Gold L1,2, Weiss J3, Rueda MJ4, Liu H5, Tanghetti E6. Am J Clin Dermatol. 2016 Mar 5. [Epub ahead of print]
BACKGROUND: A need exists for topical treatments in managing more severe inflammatory acne.