ITX5061

• CAT Number: I007402
• CAS Number: 1252679-52-9
• Molecular Formula: C30H38ClN3O7S
• Molecular Weight: 620.16
• Purity: ≥95%
• Synonyms: N-[5-tert-butyl-3-(methanesulfonamido)-2-methoxyphenyl]-2-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]-2-oxoacetamide;hydrochloride
• InChI: InChI=1S/C30H37N3O7S.ClH/c1-30(2,3)20-18-24(28(38-4)25(19-20)32-41(5,36)37)31-29(35)27(34)23-10-11-26(22-9-7-6-8-21(22)23)40-17-14-33-12-15-39-16-13-33;/h6-11,18-19,32H,12-17H2,1-5H3,(H,31,35);1H
• InChIKey: ICIJBYYMEBOTQP-UHFFFAOYSA-N
• SMILES: CC(C)(C)C1=CC(=C(C(=C1)NS(=O)(=O)C)OC)NC(=O)C(=O)C2=CC=C(C3=CC=CC=C32)OCCN4CCOCC4.Cl

ITX5061 is a type II inhibitor of p38 MAPK and also an antagonist of scavenger receptor B1 (SR-B1).
ITX5061 is a type II inhibitor of p38 MAPK and also an antagonist of scavenger receptor B1 (SR-B1). Treatment of ITX5061 (30 mg/kg/day) for mice results in a 50% increase in HDL-C levels compare to baseline. ApoA-I levels are moderately (+15 %) but significantly increased in ITX5061-treated HuAITg mice, compare to mice receive vehicle. ITX5061 significantly decreases HDL-CE catabolism with an FCR of 1.86±0.40 pools/d vs 2.47±0.26 pools/d in the control group (P<0.05), while calculated production rates are identical in both groups (129±24 μg/g/d vs 129±16 μg/g/d). Moreover, accumulation of [3H] CE in the liver is significantly lower in ITX5061-treated mice indicating that increased HDL-CE levels are due to reduced uptake by the liver[1].

Reference

[1]. Masson D, et al. Increased HDL cholesterol and apoA-I in humans and mice treated with a novel SR-BI inhibitor. Arterioscler Thromb Vasc Biol. 2009 Dec;29(12):2054-60.
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