ITX5061 free base
Based on 3 publication(s) in Google Scholar
ITX5061 free base is an orally active type II non-competitive p38 MAPK inhibitor. ITX5061 free base increases HDL-C levels by inhibiting SR-BI activity. ITX5061 free base also moderately elevates ApoA-I levels. ITX5061 free base reduces early atherosclerotic lesions in the aortic arch of mice fed an atherogenic diet. ITX5061 free base can be used in the research of atherosclerosis.
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- CAS No.: 848144-15-0
- Formule: C30H37N3O7S
- Masse moléculaire:583.70
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Publications Citing Use of MedChemExpress (MCE) ITX5061 free base
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
0.77 μM
Compound: ITX-5061
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Inhibition of mouse SR-BI isoform 1 expressed in CHO cells assessed as reduction in uptake of [3H]CE from [3H]CE-HDL by by liquid scintillation counting method
Inhibition of mouse SR-BI isoform 1 expressed in CHO cells assessed as reduction in uptake of [3H]CE from [3H]CE-HDL by by liquid scintillation counting method
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[PMID: 25958245] |
In Vitro
ITX5061 (1 μM) free base 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) free base 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) free base 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.
Chemical Information
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CAS No. 848144-15-0
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Masse moléculaire 583.70
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Formule C30H37N3O7S
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SMILES
O=C(NC=1C=C(C=C(NS(=O)(=O)C)C1OC)C(C)(C)C)C(=O)C2=CC=C(OCCN3CCOCC3)C=4C=CC=CC24
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
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 -
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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