ITX5061 |
Katalog-Nr.GC32209 |
ITX5061 ist ein Typ-II-Inhibitor von p38 MAPK und auch ein Antagonist des Scavenger-Rezeptors B1 (SR-B1).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1252679-52-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. |
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.
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. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Average Rating: 5
(Based on Reviews and 24 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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