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TAK-906

Cat. No. M21180
TAK-906 Structure
Synonym:

Trazpiroben

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Quality Control & Documentation
Biological Activity

TAK-906 is a peripherally restricted, non-BBB permeable molecule that targets the posterior region of the stomach and vomiting center for the study of gastric cramps.

Chemical Information
Molecular Weight 517.66
Formula C31H39N3O4
CAS Number 1352993-39-5
Solubility (25°C) N/A
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] Jatinder K Mukker, et al. Clin Transl Sci. The pharmacokinetics of oral trazpiroben (TAK-906) after organic anion transporting polypeptide 1B1/1B3 inhibition: A phase I, randomized study

[2] Jatinder Kaur Mukker, et al. Clin Transl Sci. Evaluation of the pharmacokinetics of trazpiroben (TAK-906) in the presence and absence of the proton pump inhibitor esomeprazole

[3] Laura Kreckler, et al. J Exp Pharmacol. Non-Clinical Safety Pharmacology Evaluations of Trazpiroben (TAK-906), a Novel Dopamine D2/D3 Selective Receptor Antagonist for the Management of Gastroparesis

[4] Mitsuhiro Nishihara, et al. Xenobiotica. Evaluation of the drug-drug interaction potential for trazpiroben (TAK-906), a D2/D3 receptor antagonist for gastroparesis, towards cytochrome P450s and transporters

[5] Roger L Whiting, et al. Clin Pharmacol Drug Dev. Safety, Pharmacokinetics, and Pharmacodynamics of Trazpiroben (TAK-906), a Novel Selective D2 /D3 Receptor Antagonist: A Phase 1 Randomized, Placebo-Controlled Single- and Multiple-Dose Escalation Study in Healthy Participants

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Keywords: TAK-906, Trazpiroben supplier, Dopamine Receptor, inhibitors, activators

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