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URAT1 inhibitor 7

Cat. No. M42270
URAT1 inhibitor 7 Structure
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Biological Activity

URAT1 inhibitor 7 is a potent URAT1 inhibitor, with an IC50 of 12 nM.

Chemical Information
Molecular Weight 428.82
Formula C19H10ClFN4O3S
CAS Number 1632002-28-8
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] Jordana Dinorá de Lima et al. Immunol Invest. Genetic and Epigenetic Regulation of the Innate Immune Response to Gout

[2] Qian Ren et al. Phytomedicine. Natural flavonol fisetin attenuated hyperuricemic nephropathy via inhibiting IL-6/JAK2/STAT3 and TGF-β/SMAD3 signaling

[3] Ze-An Zhao et al. Acta Pharmacol Sin. CDER167, a dual inhibitor of URAT1 and GLUT9, is a novel and potent uricosuric candidate for the treatment of hyperuricemia

[4] Thomas Bardin et al. Rheumatology (Oxford). Novel uricosurics

[5] Hiroshi Miyata et al. Front Pharmacol. Identification of Febuxostat as a New Strong ABCG2 Inhibitor: Potential Applications and Risks in Clinical Situations

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