ITX-5061 hydrochloride

Research use only, not for human use.

ITX-5061 is a scavenger receptor B1 antagonist that promotes high-density lipoprotein (HDL) levels.

ITX-5061 is a scavenger receptor B1 antagonist that promotes high-density lipoprotein (HDL) levels; inhibits SR-BI-dependent uptake of HDL-CE in transfected cells, decreases the fractional catabolic rate of HDL-CE and reduced its hepatic uptake in mice; inhibits HCVcc and HCVpp infection of primary human hepatocytes and/or human hepatoma cell lines and has minimal effects on HCV RNA replication.HCV Infection Phase 2 Clinical.

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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.

ITX5061

Immunology/Inflammation

Scavenger Receptor

Scavenger Receptor

Infection

HCV Infection

1252679-52-9

620.158

C30H38ClN3O7S

>98% (HPLC)

DMSO : ≥ 83.3 mg/mL 134.32 mM

O=C(NC1=CC(C(C)(C)C)=CC(NS(=O)(C)=O)=C1OC)C(C2=C3C=CC=CC3=C(OCCN4CCOCC4)C=C2)=O.[H]Cl

N-(5-(tert-butyl)-2-methoxy-3-(methylsulfonamido)phenyl)-2-(4-(2-morpholinoethoxy)naphthalen-1-yl)-2-oxoacetamide hydrochloride

(-20℃)

With Ice Pack

≥ 2 years