An MC4R antagonist
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HS-014 (trifluoroacetate salt)

Item No. 41556

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
cyclic (1→8)-disulfide N-acetyl-L-cysteinyl-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, trifluoroacetate salt
Synonyms
  • Cyclic [Ac-Cys11, D-Nal14, Cys18, Asp-NH2]-β-MSH(11-22)
Molecular Formula
C71H94N20O17S2 • XCF3COOH
Formula Weight
1563.8
Purity
≥98%
Formulation (Request formulation change)
A solid
Peptide Sequence
Ac-CEHXRWGCPPKD-NH2 (X = 3-(2-naphthyl)-alanine)
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlPBS (pH 7.2): Soluble: ≥10 mg/ml
SMILES
O=C([C@@H](NC([C@H](NC([C@@H](NC([C@@H](NC([C@H](CSSC[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)NC(C)=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.O=C(O)C(F)(F)F
InChi Code
InChI=1S/C71H94N20O17S2.C2HF3O2/c1-38(92)81-53-35-109-110-36-54(69(107)91-26-10-18-56(91)70(108)90-25-9-17-55(90)68(106)85-46(15-6-7-23-72)62(100)86-49(60(73)98)31-59(96)97)82-57(93)34-79-61(99)51(29-42-32-78-45-14-5-4-13-44(42)45)88-63(101)47(16-8-24-77-71(74)75)83-65(103)50(28-39-19-20-40-11-2-3-12-41(40)27-39)87-66(104)52(30-43-33-76-37-80-43)89-64(102)48(84-67(53)105)21-22-58(94)95;3-2(4,5)1(6)7/h2-5,11-14,19-20,27,32-33,37,46-56,78H,6-10,15-18,21-26,28-31,34-36,72H2,1H3,(H2,73,98)(H,76,80)(H,79,99)(H,81,92)(H,82,93)(H,83,103)(H,84,105)(H,85,106)(H,86,100)(H,87,104)(H,88,101)(H,89,102)(H,94,95)(H,96,97)(H4,74,75,77);(H,6,7)/t46-,47-,48-,49-,50+,51-,52-,53-,54-,55-,56-;/m0./s1
InChi Key
XFWXDSGIBQHHGQ-FNAFJDLNSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    HS-014 is an antagonist of melanocortin receptor 4 (MC4R; Ki = 3.16 nM).1 It is selective for MC4R over MC1R, MC3R, and MC5R (Kis = 108, 54.4, and 694 nM, respectively). HS-014 inhibits cAMP accumulation induced by α-melanocyte-stimulating hormone (α-MSH) in COS-1 cells expressing MC4R in a concentration-dependent manner. It increases food intake in free-feeding rats when administered intracerebroventricularly at doses of 1 or 3 nmol/animal.2 Intracerebroventricular administration of HS-014 (0.008 ng/animal) increases the latency to tail withdrawal in the tail-flick test, as well as inhibits morphine withdrawal-induced decreases in the latency to tail withdrawal in the tail-flick test, in rats.3 It reduces immobility time in the forced swim test, as well as increases time in the open area and reduces the number of droppings in an open field test, in rats when administered at a dose of 100 µg/animal.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schiöth, H.B., Mutulis, F., Muceniece, R., et al. Discovery of novel melanocortin4 receptor selective MSH analogues. Br. J. Pharmacol. 124(1), 75-82 (1998).

    2. Kask, A., Rägo, L., Mutulis, F., et al. Selective antagonist for the melanocortin 4 receptor (HS014) increases food intake in free-feeding rats. Biochem. Biophys. Res. Commun. 245(1), 90-93 (1998).

    3. Kalange, A.S., Kokare, D.M., Singru, P.S., et al. Central administration of selective melanocortin 4 receptor antagonist HS014 prevents morphine tolerance and withdrawal hyperalgesia. Brain Res. 1181, 10-20 (2007).

    4. Serova, L.I., Laukova, M., Alaluf, L.G., et al. Intranasal infusion of melanocortin receptor four (MC4R) antagonist to rats ameliorates development of depression and anxiety related symptoms induced by single prolonged stress. Behav. Brain Res. 250, 139-147 (2013).