o-demethyl apremilast

O-Demethyl apremilast is an active metabolite of the phosphodiesterase 4 (PDE4) inhibitor apremilast .1It inhibits the activity of PDE4 isolated from U937 cells and LPS-induced TNF-α production in isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 8.3 and 5.6 μM, respectively). O-Demethyl apremilast is also an oxidative degradation product of apremilast.2,3 1.Hoffmann, M., Kumar, G., Schafer, P., et al.Disposition, metabolism and mass balance of [14C]apremilast following oral administrationXenobiotica41(12)1063-1075(2011) 2.Lu, Y., Shen, X., Hang, T., et al.Identification and characterization of process-related substances and degradation products in apremilast: Process optimization and degradation pathway elucidationJ. Pharm. Biomed. Anal.14170-78(2017) 3.Bhole, R.P., Naksakhare, S.R., and Bonde, C.G.A stability indicating HPTLC method for apremilast and identification of degradation products using MS/MSJ. Pharm. Sci. & Res.11(5)1861-1869(2019)

Novolimus is a macrocyclic lactone with anti-proliferative properties. It has similar efficacy to currently available agents but requires a lower dose.

20-O-Demethyl-AP3 is a secondary metabolite derived from Ansamitocin P-3, and Ansamitocin P-3 is a macrocyclic antitumor antibiotic exerting its therapeutic effects by inhibiting microtubules.

8-O-Demethyl-7-O-methyl-3,9-dihydropunctatin is a natural product for research related to life sciences. The catalog number is TN3290 and the CAS number is 93078-83-2.

O-Demethyl Lenvatinib, a metabolite of Lenvatinib (E7080), is an orally administered, multi-targeted tyrosine kinase inhibitor. It effectively inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, demonstrating significant antitumor activities [1] [2].

O-Demethyl Lenvatinib hydrochloride, a metabolite of Lenvatinib (E7080), is an orally administered multi-targeted tyrosine kinase inhibitor. It targets and inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, demonstrating potent antitumor activities [1] [2].

O-Demethyl apixaban sulfate is a metabolite of Apixaban, a potent and highly selective factor Xa inhibitor. Apixaban is currently under development for treatment of arterial and venous thrombotic diseases.

6-O-demethyl Griseofulvin is a metabolite of the antifungal griseofulvin .1,2