2. MAPK/ERK Pathway Immunology/Inflammation
  3. p38 MAPK Scavenger Receptor Class B type I (SR-BI）
  4. ITX5061 free base

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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ITX5061 free base

ITX5061 free base Chemical Structure

CAS No. : 848144-15-0

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ITX5061 free base Related Antibodies

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Description

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[1].

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.

ITX5061 free base Related Antibodies
In Vivo

ITX5061 (30 mg/kg; daily; 7 days) free base increases HDL-C and apoA-I levels, shifts HDL to larger particles, and reduces HDL-CE catabolism and hepatic uptake in HuAITg mice, with a 50% increase in HDL-C and 15% increase in apoA-I after one week of treatment[1].
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.

Animal Model: C57Bl/6 human apoA-I transgenic (HuAITg)[1]
Dosage: 30 mg/kg
Administration: daily; 7 days
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.
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]
Dosage: 0.037% incorporated into diet
Administration: daily; 18 weeks
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.
Molecular Weight

583.70

Formula

C30H37N3O7S
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ITX5061 free base Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ITX5061848144-15-0ITX 5061ITX-5061p38 MAPKScavenger Receptor Class B type I (SR-BI）Scavenger receptor class B member 1SRB1CD36 and LIMPII analogous 1 (CLA-1)CD36 antigen-like 1HDL-CSR-BI-deficient miceWT miceHuAITg miceatherosclerosisLdlr+/? micep38 MAPK type IIHEK 293 cellsapoA-ISR-BIInhibitorinhibitorinhibit

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