An MC4R antagonist
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JKC363 (acetate)

Item No. 41555

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
cyclic (1→7)-disulfide N-(3-mercapto-1-oxopropyl)-L-α-glutamyl-L-histidyl-3-(2-naphthalenyl)-D-alanyl-L-arginyl-L-tryptophylglycyl-L-cysteinyl-L-prolyl-L-prolyl-L-lysyl-L-α-asparagine, acetate
Synonyms
  • Ac-c[Deamino-Cys11-D-Nal14-Cys18-Asp22]-β-MSH-(11-22)-NH2
  • Cyclic [Mpr11,D-Nal14,Cys18,Asp22-NH2]-β-MSH (11-22)
Molecular Formula
C69H91N19O16S2 • XC2H4O2
Formula Weight
1506.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Peptide Sequence
cyclo(X1EHx2RWGC)PPKD-NH2 (X1=β-mercaptopropionate; x2=β-(2-naphthyl)-D-alanine)
Solubility(Learn about Variance in Solubility)
PBS (pH 7.2): Soluble: ≥10 mg/ml
SMILES
O=C([C@@H](NC([C@H](NC([C@@H](NC([C@@H](NC(CCSSC[C@H](NC(CNC1=O)=O)C(N2[C@@H](CCC2)C(N3[C@@H](CCC3)C(N[C@@H](CCCCN)C(N[C@H](C(N)=O)CC(O)=O)=O)=O)=O)=O)=O)CCC(O)=O)=O)CC4=CN=CN4)=O)CC5=CC6=C(C=CC=C6)C=C5)=O)CCCNC(N)=N)N[C@H]1CC7=CNC8=CC=CC=C78.CC(O)=O
InChi Code
InChI=1S/C69H91N19O16S2.C2H4O2/c70-23-6-5-14-45(61(97)83-48(59(71)95)32-58(93)94)82-66(102)53-16-8-25-87(53)68(104)54-17-9-26-88(54)67(103)52-36-106-105-27-22-55(89)79-47(20-21-57(91)92)63(99)86-51(31-42-34-74-37-78-42)65(101)84-49(29-38-18-19-39-10-1-2-11-40(39)28-38)64(100)81-46(15-7-24-75-69(72)73)62(98)85-50(60(96)77-35-56(90)80-52)30-41-33-76-44-13-4-3-12-43(41)44;1-2(3)4/h1-4,10-13,18-19,28,33-34,37,45-54,76H,5-9,14-17,20-27,29-32,35-36,70H2,(H2,71,95)(H,74,78)(H,77,96)(H,79,89)(H,80,90)(H,81,100)(H,82,102)(H,83,97)(H,84,101)(H,85,98)(H,86,99)(H,91,92)(H,93,94)(H4,72,73,75);1H3,(H,3,4)/t45-,46-,47-,48-,49+,50-,51-,52-,53-,54-;/m0./s1
InChi Key
IJVLUTUXDRKUQF-FVOJPQBCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    25 mg

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    Product Description

    JKC363 is a cyclic peptide antagonist of melanocortin receptor 4 (MC4R) (IC50 = 0.5 nM).1 It is selective for MC4R over MC3R (IC50 = 44.9 nM). JKC363 (100 nM) decreases basal thyrotropin-releasing hormone (TRH) secretion and α-melanocyte-stimulating hormone- (α-MSH-) or γ2-MSH-induced TRH secretion in rat hypothalamic explants. It inhibits proliferation of isolated postnatal rat hippocampal neural precursor cells induced by [Nle4,D-Phe7]-α-MSH (Item No. 41548) when used at a concentration of 10 nM.2 Intrathecal administration of JKC363 (5 nmol/animal) decreases paw licking and flinching in the formalin test in mice.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kim, M.S., Small, C.J., Russell, S.H., et al. Effects of melanocortin receptor ligands on thyrotropin-releasing hormone release: Evidence for the differential roles of melanocortin 3 and 4 receptors. J. Neuroendocrinol. 14(4), 276-282 (2002).

    2. Carniglia, L., Turati, J., Saba, J., et al. Melanocortin-receptor 4 activation modulates proliferation and differentiation of rat postnatal hippocampal neural precursor cells. Neuropharmacology 257, 110058 (2024).

    3. Bellasio, S., Nicolussi, E., Bertorelli, R., et al. Melanocortin receptor agonists and antagonists modulate nociceptive sensitivity in the mouse formalin test. Eur. J. Pharmacol. 482(1-3), 127-132 (2003).