A synthetic retinoid; an agonist of RARs (Kds = 1

Adapalene – 500 mg

Brand:
Cayman
CAS:
106685-40-9
Storage:
-20
UN-No:
Non-Hazardous - /

Adapalene is a synthetic retinoid and an agonist of retinoic acid receptors (RARs; Kds = 1,100, 34, and 130 nM for RARα, RARβ, and RARγ, respectively).{18516,37761,37762,37763,37764} It inhibits growth and differentiation of sebocytes in a concentration-dependent manner in primary rat preputial cell culture. Adapalene (10 μM) completely inhibits the activity of soybean 15-lipoxygenase (15-LOX) in an enzyme assay and inhibits the 5- and 15-LOX pathways in human blood polymorphonuclear leukocytes (PMNs).{37761} It reduces the protein levels of toll-like receptor 2 (TLR2) and IL-10 in skin explants isolated from patients with acne and healthy controls in a concentration-dependent manner but increases the expression of the antigen-presenting protein CD1d in acne skin explants while decreasing it in control explants.{37762} It inhibits inflammation in rodent models of ear edema induced by arachidonic acid and carrageenan-induced paw edema.{37761} Adapalene (100 μM) also induces apoptosis and inhibits proliferation of CC-531, HT-29, and LoVo colon cancer cells and reduces tumor growth in a DLD-1 colon cancer nude mouse xenograft model in a dose-dependent manner.{37764,37763} Formulations containing adapalene have been used in the treatment of acne vulgaris.  

 

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Description

A synthetic retinoid; an agonist of RARs (Kds = 1,100, 34, and 130 nM for RARα, RARβ, and RARγ, respectively); inhibits growth and differentiation of sebocytes in primary rat preputial cell culture; completely inhibits the activity of soybean 15-LOX in an enzyme assay at 10 μM; inhibits the 5- and 15-LOX pathways in human blood PMNs at 10 μM; reduces the protein levels of TLR2 and IL-10 in skin explants isolated from patients with acne as well as healthy controls; increases the expression of CD1d in acne skin explants while decreasing it in control explants; inhibits inflammation in rodent models of ear edema induced by arachidonic acid and carrageenan-induced paw edema; induces apoptosis and inhibits proliferation of CC-531, HT-29, and LoVo colon cancer cells at 100 μM; reduces tumor growth in a DLD-1 colon cancer nude mouse xenograft model

Formal name: 6-(4-methoxy-3-tricyclo[3.3.1.13,7]dec-1-ylphenyl)-2-naphthalenecarboxylic acid

Synonyms:  CD 271

Molecular weight: 412.5

CAS: 106685-40-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Small Molecule Inhibitors|Lipoxygenases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Endocrinology & Metabolism|Hormones & Receptors|RARs, RORs, & RXRs||Research Area|Immunology & Inflammation|Innate Immunity|Pattern Recognition||Research Area|Lipid Biochemistry|Lipoxygenase Pathways

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