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Adapalene
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Adapalene图片
CAS NO:106685-40-9
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议
5g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)412.52
FormulaC28H28O3
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
SMILES Code COC1=C(C=C(C=C1)C2=CC3=C(C=C2)C=C(C=C3)C(=O)O)C45CC6CC(C4)CC(C6)C5
SynonymsDifferin; Adaferin; CD271; Adapaleno; ADAPALENE; Adapalenum; CD-271; CD 271.
实验参考方法
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.


Cell Assay: 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.

In VivoAdapalene 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 modelRhino mice.
Formulation & DosageN/A
References

Drugs. 1997 Mar;53(3):511-9; Exp Dermatol. 2007 Jun;16(6):500-6.