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ZL0420

Cat. No. M10908
ZL0420  Structure
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Biological Activity

ZL0420 is a potent and selective BET bromine domain 4 (BRD4) inhibitor of BRD4 BD1 and BRD4 BD2 IC50 27 nM and 32 nM, respectively.

Chemical Information
Molecular Weight 296.32
Formula C16H16N4O2
CAS Number 2230496-80-5
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Xi Lu, et al. Ecotoxicol Environ Saf. Novel insights into the role of BRD4 in fine particulate matter induced airway hyperresponsiveness

[2] Bing Tian, et al. Am J Respir Cell Mol Biol. Efficacy of Novel Highly Specific Bromodomain-Containing Protein 4 Inhibitors in Innate Inflammation-Driven Airway Remodeling

[3] Zhiqing Liu, et al. Eur J Med Chem. Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation

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  Catalog
Abmole Inhibitor Catalog




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