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Trifluoperazine N-Glucuronide

Cat. No. M28780
Trifluoperazine N-Glucuronide Structure
Synonym:

UGT1A4

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Biological Activity

Trifluoperazine N-Glucuronide (UGT1A4), as one of the human UGT1A isoforms, is expressed in the liver. Trifluoperazine N-Glucuronide catalyzes the imipramine and trifluoperazine Nglucuronide formation.

Chemical Information
Molecular Weight 583.62
Formula C27H32F3N3O6S
CAS Number 165602-90-4
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Zhe Wang, et al. Curr Drug Metab. Cabozantinib Carries the Risk of Drug-Drug Interactions via Inhibition of UDPglucuronosyltransferase (UGT) 1A9

[2] Jian Guo, et al. J Pharm Biomed Anal. Liquid chromatography-tandem mass spectrometry method for measurement of nicotine N-glucuronide: a marker for human UGT2B10 inhibition

[3] Ryoichi Fujiwara, et al. Drug Metab Dispos. Interactions between human UGT1A1, UGT1A4, and UGT1A6 affect their enzymatic activities

[4] Hidefumi Kaji, et al. Drug Metab Dispos. Characterization of afloqualone N-glucuronidation: species differences and identification of human UDP-glucuronosyltransferase isoform(s)

[5] Omar Ghosheh, et al. Drug Metab Dispos. N-glucuronidation of nicotine and cotinine in human: formation of cotinine glucuronide in liver microsomes and lack of catalysis by 10 examined UDP-glucuronosyltransferases

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