Screening analogs of the cyclic lactam melanocortin agonist MTII led to the identification of the agoutimimetic SHU9119. This compound shares pharmacological properties with the agouti peptide in that it is a potent antagonist of the melanocortin-4 receptor and a less potent antagonist of the melanocortin-3 receptor.
HS028 (cyclic [AcCys11, dichloro-D-phenylalanine14, Cys18, Asp-NH2(22)]-beta-MSH11-22) showed high affinity (Ki of 0.95nM) and high (80 fold) MC4 receptor selectivity over the MC3 receptor. HS028 antagonised a alpha-MSH induced increase in cyclic AMP production in transfected cells expressing the MC3 and MC4 receptors, whereas it seemed to be a partial agonist for the MC1 and MC5 receptors. Chronic intracerebroventricularly (i.c.v.) administration of HS028 by osmotic minipumps significantly increased both food intake and body weight in a dose dependent manner without tachyphylaxis for a period of 7 days. This is further evidence that the MC4 receptor is an important mediator of long term weight homeostasis.
[D-Trp7, Ala8, D-Phe10]-α-Melanocyte Stimulating Hormone Amide Fragment 6-11 ≥97% (HPLC)
Selective inhibitor of α-MSH activity in frog skin bioassay; identical to (His1,Lys8)-GH which selectively releases growth hormone in vitro and in vivo; somatostatin antagonist.
[Met210]-Melanocyte Protein PMEL 17 Fragment 209-217 human, mouse >98% (HPLC), solid
Modification of the melanoma differentiation antigen gp100/PMEL 17 fragment 209-217 sequence with greater affinity for the HLA-A2 molecule than the unmodified peptide. Has an increased ability to generate melanoma-reactive cytotoxic T lymphocytes in vitro.
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