1. MAPK/ERK Pathway
  2. p38 MAPK

ITX5061 

Cat. No.: HY-19900 Purity: 98.07%
Handling Instructions

ITX5061 is a type II inhibitor of p38 MAPK and also an antagonist of scavenger receptor B1 (SR-B1).

For research use only. We do not sell to patients.

ITX5061 Chemical Structure

ITX5061 Chemical Structure

CAS No. : 1252679-52-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 2460 In-stock
Estimated Time of Arrival: December 31
1 mg USD 1127 In-stock
Estimated Time of Arrival: December 31
5 mg USD 1803 In-stock
Estimated Time of Arrival: December 31
10 mg USD 2885 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

ITX5061 is a type II inhibitor of p38 MAPK and also an antagonist of scavenger receptor B1 (SR-B1).

IC50 & Target

p38 MAPK, SR-B1[1]

In Vivo

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].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 83.3 mg/mL (134.32 mM)

*"≥" 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
10 mM 0.1612 mL 0.8062 mL 1.6125 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

620.16

Formula

C₃₀H₃₈ClN₃O₇S

CAS No.

1252679-52-9

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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ITX5061
Cat. No.:
HY-19900
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ITX5061

Cat. No.: HY-19900