ITX-5061 HCl
ITX-5061 HCl Basic information
- Product Name:
- ITX-5061 HCl
- Synonyms:
-
- ITX-5061 HCl
- ITX-5061
- ITX-5061 hydrochloride (ITX5061)
- ITX-5061 hydrochloride
- ITX506 HCl
- N-(5-(tert-Butyl)-2-methoxy-3-(methylsulfonamido)phenyl)-2-(4-(2-morpholinoethoxy)naphthalen-1-yl)-2-oxoacetamide hydrochloride , ITX5061
- N-(5-(tert-Butyl)-2-methoxy-3-(methylsulfonamido)phenyl)-2-(4-(2-morpholinoethoxy)naphthalen-1-yl)-2-oxoacetamide hydrochloride
- CAS:
- 1252679-52-9
- MF:
- C30H38ClN3O7S
- MW:
- 620.16
- Mol File:
- 1252679-52-9.mol
ITX-5061 HCl Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO : ≥ 83.3 mg/mL (134.32 mM)
- form
- Solid
- color
- Light yellow to light brown
ITX-5061 HCl Usage And Synthesis
Uses
ITX5061 is a type II inhibitor of p38 MAPK and also an antagonist of scavenger receptor B1 (SR-B1).
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].
References
[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. DOI:10.1161/ATVBAHA.109.191320
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