RO27-3225 TFA

RO27-3225, also known as RO273225 is a melanocortin type 4 receptor agonist with EC50 = 1 nM. It may alleviate intestinal dysfuntion and brain damage. It has been investigated for an anti-obesity medication. Ro 27-3225 shows some activity at the MC1 receptor. Ro 27-3225 reverses hemorrhagic shock, reduces multiple organ damage, and improves survival.

RO27-3225 trifluoroacetate is a peptide agonist of melanocortin receptor 4 (MC4R) with neuroprotective and anti-inflammatory activity with an EC50 value of 1 nM, while 8 nM for MC1R. RO27-3225 trifluoroacetate reverses hemorrhagic shock, reduces brain edema, blood-brain barrier (BBB) permeability, and hippocampal IL-1β and TNF-α levels in a rat model of intra-abdominal hypertension induced by hemorrhagic shock and resuscitation[1][2].

MC4R: 1 nM (EC₅₀); MC1R: 8 nM (EC₅₀)

[1] Liu D, et al. Melanocortin MC4 receptor agonists alleviate brain damage in abdominal compartment syndrome in the rat. Neuropeptides. 2015 Feb;49:55-61. DOI:10.1016/j.npep.2014.12.003
[2] Benoit SC, et al. A novel selective melanocortin-4 receptor agonist reduces food intake in rats and mice without producing aversive consequences. J Neurosci. 2000 May 1;20(9):3442-8. DOI:10.1523/JNEUROSCI.20-09-03442.2000