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TRV250

Cat. No. M31390
TRV250 Structure
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Biological Activity

TRV250 is a novel delta-like opioid receptor (DOR) small molecule agonist that preferentially selects G-protein signaling with relatively little activation of the β-arrestin2 post-receptor signaling pathway.

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] Michael J Fossler, et al. CNS Drugs. A Phase I, Randomized, Single‑Blind, Placebo‑Controlled, Single Ascending Dose Study of the Safety, Tolerability, and Pharmacokinetics of Subcutaneous and Oral TRV250, a G Protein-Selective Delta Receptor Agonist, in Healthy Subjects

[2] Camden Hebson, et al. J Pediatr Hematol Oncol. Elevated tricuspid regurgitant velocity as a marker for pulmonary hypertension in children with sickle cell disease: less prevalent and predictive than previously thought?

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  Catalog
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Keywords: TRV250 supplier, Opioid Receptor, inhibitors, activators


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