ITX5061
Based on 3 publication(s) in Google Scholar
ITX5061 is an orally active type II non-competitive p38 MAPK inhibitor. ITX5061 increases HDL-C levels by inhibiting SR-BI activity. ITX5061 also moderately elevates ApoA-I levels. ITX5061 reduces early atherosclerotic lesions in the aortic arch of mice fed an atherogenic diet. ITX5061 can be used in the research of atherosclerosis.
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- Pureza: 99.69%
- No. CAS: 1252679-52-9
- Fòrmula: C30H38ClN3O7S
- Peso molecular:620.16
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) ITX5061
More
Actividad biológica
Descripciòn
IC50 & Target
p38 MAPK, SR-B1[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.77 μM
Compound: ITX-5061
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Inhibition of mouse SR-B1 overexpressed in CHO cells assessed as inhibition of [3H]cholesteryl ester uptake into cells after 2 to 3 hrs by liquid scintillation counting
Inhibition of mouse SR-B1 overexpressed in CHO cells assessed as inhibition of [3H]cholesteryl ester uptake into cells after 2 to 3 hrs by liquid scintillation counting
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[PMID: 25900219] |
In Vitro
ITX5061 (1 μM) significantly inhibits SR-BI-mediated HDL uptake in HEK 293 cells overexpressing SR-BI[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
ITX5061 (30 mg/kg; daily; 7 days) increases HDL-C levels in WT mice in an SR-BI-dependent manner, with no effect on HDL-C in SR-BI−/− mice[1].
ITX5061 (0.037% incorporated into diet; daily; 18 weeks) increases HDL-C by 30% and reduces early atherosclerotic lesions in the aortic arch by 40% in Ldlr+/− mice fed a Paigen diet for 18 weeks, regardless of CETP expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl/6 human apoA-I transgenic (HuAITg)[1]
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Dosage:30 mg/kg
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Administration:daily; 7 days
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Result:Increased HDL-C levels by 50% compared to baseline.
Did not change non-HDL-C levels.
Increased apoA-I levels by 15% compared to vehicle controls.
Induced a shift towards larger-sized HDL.
Decreased HDL-CE fractional catabolic rate to 1.86 pools/d (vs 2.47 pools/d in controls, P<0.05).
Kept HDL-CE production rates identical to controls at 129 μg/g/d.
Reduced accumulation of [3H] CE in the liver significantly.
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Animal Model:F1 hybrid C57BL/6 × DBA/1 Ldlr+/− (with or without CETP expression induced by AAV-CETP injection; fed Paigen high-fat/cholesterol/bile salt diet for 18 weeks)[1]
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Dosage:0.037% incorporated into diet
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Administration:daily; 18 weeks
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Result:Increased HDL-C concentrations by 30%.
Showed no differences in total cholesterol or triglyceride levels compared to controls.
Reduced early atherosclerotic lesions in the aortic arch by 40% (both with and without CETP expression).
Showed a non-significant trend towards reduced lesion area in the aortic valves.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1252679-52-9
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Appearance Solid
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Peso molecular 620.16
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Fòrmula C30H38ClN3O7S
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Color Light yellow to light brown
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Metab
2020 Dec;2(12):1391-1400. PMID: 33244168 -
iScience
The HDL-transporting scavenger receptor B1 promotes viral infection through endolysosomal acidification. [Abstract]2025 Apr 24;28(6):112501. PMID: 40475258 -
Solvente y solubilidad
In Vitro:
DMSO : ≥ 83.3 mg/mL (134.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6125 mL | 8.0624 mL | 16.1249 mL | 40.3122 mL |
| 5 mM | 0.3225 mL | 1.6125 mL | 3.2250 mL | 8.0624 mL | |
| 10 mM | 0.1612 mL | 0.8062 mL | 1.6125 mL | 4.0312 mL | |
| 15 mM | 0.1075 mL | 0.5375 mL | 1.0750 mL | 2.6875 mL | |
| 20 mM | 0.0806 mL | 0.4031 mL | 0.8062 mL | 2.0156 mL | |
| 25 mM | 0.0645 mL | 0.3225 mL | 0.6450 mL | 1.6125 mL | |
| 30 mM | 0.0537 mL | 0.2687 mL | 0.5375 mL | 1.3437 mL | |
| 40 mM | 0.0403 mL | 0.2016 mL | 0.4031 mL | 1.0078 mL | |
| 50 mM | 0.0322 mL | 0.1612 mL | 0.3225 mL | 0.8062 mL | |
| 60 mM | 0.0269 mL | 0.1344 mL | 0.2687 mL | 0.6719 mL | |
| 80 mM | 0.0202 mL | 0.1008 mL | 0.2016 mL | 0.5039 mL | |
| 100 mM | 0.0161 mL | 0.0806 mL | 0.1612 mL | 0.4031 mL |
ITX5061 Related Classifications
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