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

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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ITX5061

ITX5061 Chemical Structure

CAS No. : 1252679-52-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 3 publication(s) in Google Scholar

Other Forms of ITX5061:

ITX5061 Related Antibodies

Top Publications Citing Use of Products

View All p38 MAPK Isoform Specific Products:

View All Isoforms
p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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Description

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[1].

IC50 & Target

p38 MAPK, SR-B1[1]
Cellular Effect
Cell Line Type Value Description References
CHO IC50
0.77 μM
Compound: ITX-5061
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
[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.

ITX5061 Related Antibodies
In Vivo

ITX5061 (30 mg/kg; daily; 7 days) 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) 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.

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.
Clinical Trial
Molecular Weight

620.16

Formula

C30H38ClN3O7S
CAS No.
Appearance

Solid

Color

Light yellow to light brown

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
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.

Preparing
Stock Solutions
Concentration Solvent Mass 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 3.2250 mL
View the 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.

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Purity & Documentation

Purity: 99.69%

SDS (393 KB)

COA (254 KB) HNMR (322 KB) RP-HPLC (254 KB) LCMS (99 KB)

Handling Instructions (2659 KB)
References

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
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ITX5061 Related Classifications

Help & FAQs
  • 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:

ITX50611252679-52-9ITX 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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