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TRV734

Cat. No. M31391
TRV734 Structure
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Biological Activity

TRV734 is an orally bioavailable G-protein-biased ligand for the μ-opioid receptor and an agonist for the μ-opioid receptor.

Chemical Information
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] Kimberly A Ramos, et al. Clin Pharmacol Drug Dev. Two-Part Phase 1 Multiple-Ascending-Dose Study to Evaluate the Safety, Tolerability, Pharmacodynamics, and Pharmacokinetics of TRV734 in Healthy Adults

[2] Ian E James, et al. Clin Pharmacol Drug Dev. A First-in-Human Clinical Study With TRV734, an Orally Bioavailable G-Protein-Biased Ligand at the μ-Opioid Receptor

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Keywords: TRV734 supplier, Opioid Receptor, inhibitors, activators


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