Acitretin-d3

Description

Acitretin-d3 is intended for use as an internal standard for the quantification of acitretin (Item No. 20853) by GC- or LC-MS. Acitretin is a retinoid and an active metabolite of the retinoid etretinate (Item No. 19878) that has antiproliferative activities.1,2 It binds to cellular retinoic acid binding protein I (CRABP-I) and CRABP-II (Kds = 3 and 15 nM, respectively, for the mouse recombinant proteins) but has low affinity for human recombinant retinoic acid receptor-retinoid X receptor (RAR-RXR) heterocomplexes.3,4 Acitretin inhibits proliferation (IC50 = 6.6 µM) and suppresses TNF-α- and IFN-γ-induced protein levels of STAT1, NF-ĸB, and RANTES in HaCaT keratinocytes when used at concentrations up to 50 µM.5 It inhibits proliferation of HL-60, SCC-4, SCC-15, and A431, but not MCF-7, cancer cells, when used at a concentration of 30 µM.1 Acitretin (20 µg per mouse) decreases the severity of psoriatic-like skin lesions in K14-VEGF transgenic mice.2 Formulations containing acitretin have been used in the treatment of psoriasis.WARNING This product is not for human or veterinary use.

References

[1] J.R. FREY  W. B  R Peck. Antiproliferative activity of retinoids, interferon α and their combination in five human transformed cell lines[J]. Cancer letters, 1991, 57 3: Pages 223-227. DOI: 10.1016/0304-3835(91)90161-a
[2] JINGANG AN . The acitretin and methotrexate combination therapy for psoriasis vulgaris achieves higher effectiveness and less liver fibrosis[J]. Pharmacological research, 2017, 121: Pages 158-168. DOI: 10.1016/j.phrs.2017.04.014
[3] ANDREW W. NORRIS . Measurement of subnanomolar retinoic acid binding affinities for cellular retinoic acid binding proteins by fluorometric titration[J]. Biochimica et Biophysica Acta (BBA) - Protein Structure and Molecular Enzymology, 1994, 1209 1: Pages 10-18. DOI: 10.1016/0167-4838(94)90130-9
[4] KAI-RONG TIAN. The Isolation and Characterization of Purified Heterocomplexes of Recombinant Retinoic Acid Receptor and Retinoid X Receptor Ligand Binding Domains†[J]. Biochemistry Biochemistry, 1997, 36 19: 5669-5676. DOI: 10.1021/bi9627020
[5] MIN ZHANG. Effects of acitretin on proliferative inhibition and RANTES production of HaCaT cells[J]. Archives of Dermatological Research, 2008, 300 10: 575-581. DOI: 10.1007/s00403-008-0872-z