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ITX5061 

Cat. No. M28043
ITX5061  Structure
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Biological Activity

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

Chemical Information
Molecular Weight 620.16
Formula C30H38ClN3O7S
CAS Number 1252679-52-9
Form Solid
Solubility (25°C) DMSO ≥ 83.3 mg/mL
Storage 4°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Rachana Patel, et al. EMBO Mol Med. Sprouty2 loss-induced IL6 drives castration-resistant prostate cancer through scavenger receptor B1

[2] Jihua Xue, et al. J Cell Mol Med. MEAN inhibits hepatitis C virus replication by interfering with a polypyrimidine tract-binding protein

[3] Ian A Rowe, et al. Liver Transpl. Effect of scavenger receptor class B type I antagonist ITX5061 in patients with hepatitis C virus infection undergoing liver transplantation

[4] Mark S Sulkowski, et al. J Infect Dis. Safety and antiviral activity of the HCV entry inhibitor ITX5061 in treatment-naive HCV-infected adults: a randomized, double-blind, phase 1b study

[5] David Masson, et al. Arterioscler Thromb Vasc Biol. Increased HDL cholesterol and apoA-I in humans and mice treated with a novel SR-BI inhibitor

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  Catalog
Abmole Inhibitor Catalog




Keywords: ITX5061  supplier, p38 MAPK, inhibitors, activators


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