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HET0016

Cat. No. M21437
HET0016  Structure
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Biological Activity

HET0016 is a highly efficient and selective inhibitor of 20-HETE synthase, with IC50 values of 17.7 nM, 12.1 nM and 20.6 nM for recombinant CYP4A1, CYP4A2 and CYP4A3, respectively. HET0016 is a selective CYP450 inhibitor that has been shown to inhibit angiogenesis and tumor growth.

Chemical Information
Molecular Weight 206.28
Formula C12H18N2O
CAS Number 339068-25-6
Solubility (25°C) DMSO : 5 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] Jie Wu, et al. Cell Death Dis. The interaction between STING and NCOA4 exacerbates lethal sepsis by orchestrating ferroptosis and inflammatory responses in macrophages

[2] Hai Liu, et al. Mol Carcinog. HET0016 attenuates the stemness of breast cancer cells through targeting CYP4Z1

[3] Thaiz F Borin, et al. PLoS One. HET0016 decreases lung metastasis from breast cancer in immune-competent mouse model

[4] Thaiz Ferraz Borin, et al. PLoS One. HET0016, a selective inhibitor of 20-HETE synthesis, decreases pro-angiogenic factors and inhibits growth of triple negative breast cancer in mice

[5] N Miyata, et al. Br J Pharmacol. HET0016, a potent and selective inhibitor of 20-HETE synthesizing enzyme

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Abmole Inhibitor Catalog




Keywords: HET0016 supplier, Cytochrome P450 (e.g. CYP17), inhibitors, activators


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