MCHR1 (GPR24) Agonist

Melanin Concentrating Hormone, salmon TFA (MCH (salmon) TFA) is a 19-amino-acid neuropeptide initially identified in the pituitary gland of teleost fish, which regulates food intake, energy balance, sleep state, and the cardiovascular system. Melanin-concentrating hormone is a ligand for an orphan G protein-coupled receptor (SLC-1/GPR24) and MCHR2.

Melanin Concentrating Hormone, salmon is a 19-amino-acid neuropeptide initially identified in the pituitary gland of teleost fish, which regulates food intake, energy balance, sleep state, and the cardiovascular system. Melanin-concentrating hormone is a ligand for an orphan G protein-coupled receptor (SLC-1/GPR24) and MCHR2.

(Phe13,Tyr19)-MCH (human, mouse, rat) is a potent SLC-1 and S643b receptor ligand. (Phe13,Tyr19)-MCH (human, mouse, rat) can be used as an agonist for SLC-1 and S643b receptor.

Ac-hMCH(6-16)-NH2 binds to and activates equally well both human MCH receptors present in the brain (non-selective agonist), with IC₅₀ values of 0.16 nM and 2.7 nM for MCH-1R and MCH-2R.

[Ala17]-MCH, a MCH analogue (HY-P1525A), is a selective ligand for MCHR₁ (K_i=0.16 nM) over MCHR₂ (K_i=34 nM). [Eu³⁺ chelate-labeled [Ala17]-MCH shows high affnity for MCHR₁ (K_d=0.37 nM) while has little demonstrable binding affnity for MCHR₂.

[Ala17]-MCH TFA, a MCH analogue (HY-P1525A), is a selective ligand for MCHR₁ (K_i=0.16 nM) over MCHR₂ (K_i=34 nM). [Eu³⁺ chelate-labeled [Ala17]-MCH shows high affnity for MCHR₁ (K_d=0.37 nM) while has little demonstrable binding affnity for MCHR₂.