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ITX5061

Katalog-Nr.GC32209

ITX5061 ist ein Typ-II-Inhibitor von p38 MAPK und auch ein Antagonist des Scavenger-Rezeptors B1 (SR-B1).

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ITX5061 Chemische Struktur

Cas No.: 1252679-52-9

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5 mg
585,00 $
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10 mg
882,00 $
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50 mg
2.700,00 $
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Animal experiment:

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:

[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.

Background

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].

[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.

Chemical Properties

Cas No. 1252679-52-9 SDF
Canonical SMILES O=C(NC1=CC(C(C)(C)C)=CC(NS(=O)(C)=O)=C1OC)C(C2=C3C=CC=CC3=C(OCCN4CCOCC4)C=C2)=O.Cl
Formula C30H38ClN3O7S M.Wt 620.16
Löslichkeit DMSO : ≥ 83.3 mg/mL (134.32 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.6125 mL 8.0624 mL 16.1249 mL
5 mM 0.3225 mL 1.6125 mL 3.225 mL
10 mM 0.1612 mL 0.8062 mL 1.6125 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 24 reference(s) in Google Scholar.)

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