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| SKU | Size | Availability |
Price | Qty |
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A409184-1ml
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1ml |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
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$147.90
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Retinoid Receptor Agonists
| Synonyms | CD-271 | 2-Naphthalenecarboxylic acid, 6-(4-methoxy-3-tricyclo[3.3.1.13,7]dec-1-ylphenyl)- |
|---|---|
| Specifications & Purity | Moligand™, 10mM in DMSO |
| Biochemical and Physiological Mechanisms | Adapalene (CD-271) is a dual RAR and RXR agonist, used in the treatment of acne. |
| Storage Temp | Store at -80°C |
| Shipped In |
Dry ice packs + Cold packs This product requires cold chain shipping. Ground and other economy services are not available. |
| Grade | Moligand™ |
| Action Type | AGONIST |
| Mechanism of action | Agonist of Retinoic acid receptor-αAgonist of Retinoic acid receptor-βAgonist of Retinoic acid receptor-γ |
| Product Description |
Information Adapalene Adapalene (CD-271) is a dual RAR and RXR agonist, used in the treatment of acne. 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. 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. cell lines: Concentrations: Incubation Time: Powder Purity:≥99% |
| ALogP | 6.279 |
|---|---|
| hba_count | 2 |
| Rotatable Bond | 4 |
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Smiles | COC1=C(C=C(C=C1)C2=CC3=C(C=C2)C=C(C=C3)C(O)=O)[C]45CC6[CH2][CH](C[CH]([CH2]6)C4)C5 |
|---|---|
| Molecular Weight | 412.52 |
| Reaxy-Rn | 7393980 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7393980&ln= |
| DMSO(mg / mL) Max Solubility | 8 |
|---|---|
| DMSO(mM) Max Solubility | 19.39 |
| Water(mg / mL) Max Solubility | <1 |