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TRV130 hydrochloride Oliceridine HCl

TRV130 hydrochloride Oliceridine HCl 1401031-39-7
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Chemical Information
Product name:TRV130 hydrochloride Oliceridine HCl Purity:98% min
CAS NO:1401031-39-7 Solubility:DMSO : ≥ 38 mg/mL (89.83 mM)
Molecular Formula:C22H30N2O2S Package:Package according to customer requirements
Molecular Weight:386.551 Storage:Store at -20℃
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Remarks
Oliceridine, also known as TRV130, is a µ- opioid receptor agonist, that is currently under evaluation in human clinical trials for the treatment of acute severe pain. It is a functionally selective μ-opioid receptor agonist developed by Trevena Inc. TRV130 elicits robust G protein signaling, with potency and efficacy similar to morphine, but with far less β-arrestin 2 recruitment and receptor internalization, it displays less adverse effects than morphine.
References

1: Soergel DG, Subach RA, Burnham N, Lark MW, James IE, Sadler BM, Skobieranda F, Violin JD, Webster LR. Biased agonism of the μ-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: A randomized, double-blind, placebo-controlled, crossover study in healthy volunteers. Pain. 2014 Sep;155(9):1829-35. doi: 10.1016/j.pain.2014.06.011. Epub 2014 Jun 19. PubMed PMID: 24954166.

2: Violin JD, Crombie AL, Soergel DG, Lark MW. Biased ligands at G-protein-coupled receptors: promise and progress. Trends Pharmacol Sci. 2014 Jul;35(7):308-16. doi: 10.1016/j.tips.2014.04.007. Epub 2014 May 28. Review. PubMed PMID: 24878326.

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