Home Metabolism Retinoid Receptor agonist Adapalene For research use only.

Adapalene

Synonyms: CD-271

Adapalene (CD-271) is a dual RAR and RXR agonist, used in the treatment of acne.

Adapalene Chemical Structure

Adapalene Chemical Structure

CAS: 106685-40-9

Selleck's Adapalene has been cited by 3 publications

Purity & Quality Control

Batch: Purity: 99.85%
99.85

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Biological Activity

Description Adapalene (CD-271) is a dual RAR and RXR agonist, used in the treatment of acne.
Targets
RARγ [1] RARβ [1] RXR [1]
In vitro
In vitro Adapalene binds to retinoic acid receptors found predominantly in the terminal differentiation zone of epidermis and is more active than tretinoin in modulating cellular differentiation. Adapalene shows greatest affinity for the subtype PARγ, found predominantly in the epidermis. Adapalene is more active than indomethacin, betamethasone valerate, tretinoin, isotretinoin or etretinate in inhibiting lipoxygease activity, but it has little activity against cyclo-oxygenase. [1] Adapalene time- and dose-dependently suppresses DNA synthesis and induces apoptosis in Colon carcinoma cell lines CC-531, HT-29 and LOVO as well as human foreskin fibroblasts. Adapalene shows significantly more effective antiproliferative and proapoptotic effects than 9-cis-retinoic acid (CRA), showing remarkable effects even at 10 μM. Adapalene disrupts DeltaPsi(m) and induces caspase-3 activity in responsive tumor cells. [2]
In Vivo
In vivo Adapalene produces a dose-related reduction in the number of epidermal comedones and an increase in comedo profile and epidermal thickness in the rhino mice. [1] Adapalene results in a decreased expression of TLR-2 and IL-10 in explants of normal skin and explants of acne. Adapalene can modulate the epidermal immune system by increasing the CD1d expression and by decreasing the IL-10 expression by keratinocytes, and these modulations can increase the interactions between dendritic cells and T lymphocytes and could strengthen the antimicrobial activity against Propionibacterium acnes. [3]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02620813 Completed Acne Vulgaris University of California Davis October 2015 Early Phase 1
NCT02442817 Completed Schizophrenia University of Nevada Reno|Augusta University March 2 2015 Phase 4
NCT01485367 Unknown status Senile Purpura Multispecialty Aesthetic Clinical Research Organization|Galderma R&D December 2011 Phase 2

Chemical lnformation & Solubility

Molecular Weight 412.52 Formula

C28H28O3
CAS No. 106685-40-9 SDF Download Adapalene SDF
Smiles COC1=C(C=C(C=C1)C2=CC3=C(C=C2)C=C(C=C3)C(=O)O)C45CC6CC(C4)CC(C6)C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 17 mg/mL ( (41.21 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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