product name Adapalene
Description: Adapalene (also known as CD-271) is a retinoic acid analog that acts as a dual RAR and RXR agonist with AC50 values of 2.2, 9.3, 22 and > 1000 nM for RARβ, RARγ, RARα and RXRα receptors respectively, it is used in the treatment of acne. Adapalene inhibits proliferation and induces apoptosis in colorectal cancer cells in vitro and displays comedolytic activity.
References: Drugs. 1997 Mar;53(3):511-9; Exp Dermatol. 2007 Jun;16(6):500-6.
412.52
Formula
C28H28O3
CAS No.
106685-40-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 8 mg/mL (19.4 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
CD-271
other peoduct :
| In Vitro |
In vitro activity: 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. 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Drugs. 1997 Mar;53(3):511-9; Exp Dermatol. 2007 Jun;16(6):500-6. |
