1252679-52-9
1252679-52-9 structure
- Name: ITX5061
- Chemical Name: N-[5-tert-butyl-3-(methanesulfonamido)-2-methoxyphenyl]-2-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]-2-oxoacetamide,hydrochloride
- CAS Number: 1252679-52-9
- Molecular Formula: C30H38ClN3O7S
- Molecular Weight: 620.15700
- Catalog: Signaling Pathways MAPK/ERK Pathway p38 MAPK
- Create Date: 2016-01-07 13:47:07
- Modify Date: 2024-01-14 17:43:36
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ITX5061 is a type II inhibitor of p38 MAPK and also an antagonist of scavenger receptor B1 (SR-B1).
| Name | N-[5-tert-butyl-3-(methanesulfonamido)-2-methoxyphenyl]-2-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]-2-oxoacetamide,hydrochloride |
|---|---|
| Synonyms | ITX5061 |
| Description | ITX5061 is a type II inhibitor of p38 MAPK and also an antagonist of scavenger receptor B1 (SR-B1). |
|---|---|
| Related Catalog | |
| Target |
p38 MAPK, SR-B1[1] |
| In Vivo | 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]. |
| Animal Admin | Atherosclerosis studies are conducted in F1 hybrid C57BL/6×DBA/1 Ldlr+/- mice fed the Paigen diet, which is high-fat/cholesterol/bile salt diet containing 1.25% cholesterol, 7.5% cocoa butter, and 0.5% cholic acid. For 18 weeks, the mice are put on the Paigen diet with or without ITX5061 at 0.037 %. CETP expression is induced by injection of adeno-associated virus (AAV)8 TBG human CETP vector two weeks before starting the Paigen diet. Doses of virus are given by IP injection[1]. |
| References |
| Molecular Formula | C30H38ClN3O7S |
|---|---|
| Molecular Weight | 620.15700 |
| Exact Mass | 619.21200 |
| PSA | 135.14000 |
| LogP | 6.59300 |
| Storage condition | 2-8℃ |