| Identification | Back Directory | [Name]
HS014 | [CAS]
207678-81-7 | [Synonyms]
HS014
mc4receptor antagonist
M.W. 1563.77 C71H94N20O17S2
Melanocortin 4 Receptor antagonist
(AC-CYS11,D-2-NAL14,CYS18)-BETA-MSH (11-22) AMIDE
Acetyl-(Cys11,D-2-Nal14,Cys18)-b-MSH (11-22) aMide
Acetyl-(Cys11,D-2-Nal14,Cys18)-β-MSH (11-22) amide
(ACETYL-CYS11-BETA-(2-NAPHTHYL)*-D-ALA14,CYS18)-BET
Acetyl-(Cys11,D-2-Nal14,Cys18)-Beta-MSH (11-22) amide
Acetyl-(Cys11,D-2-Nal14,Cys18)-β-MSH (11-22) aMide
HS014
(Ac-Cys11,D-Ala(2-naphthyl)14,Cys18)-b-MSH (11-22) amide
AC-CYS-GLU-HIS-D-2-NAL-ARG-TRP-GLY-CYS-PRO-PRO-LYS-ASP-NH2
AC-CYS-GLU-HIS-D-NAL(2)-ARG-TRP-GLY-CYS-PRO-PRO-LYS-ASP-NH2
(AC-CYS11,D-ALA(2-NAPHTHYL)14,CYS18)-BETA-MSH (11-22) AMIDE
MC4 Receptor antagonist, Melanocortin 4 Receptor antagonist
Ac-Cys-Glu-His-D-Nal(2)-Arg-Trp-Gly-Cys-Pro-Pro-Lys-Asp-NH2 (Disulfide bridge Cys1-Cys8)
[acetyl-cys11, β-(2-naphthyl)-d-ala14, cys18]-β-melanocyte stimulating hormone fragment 11-22
[ACETYL-CYS11, B-(2-NAPHTHYL)-D-ALA14, CYS18]-BETA-MELANOCYTE STIMULATING HORMONE FRAGMENT 11-22
L-α-Asparagine, 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-, cyclic (1→8)-disulfide | [Molecular Formula]
C71H94N20O17S2 | [MDL Number]
MFCD02179654 | [MOL File]
207678-81-7.mol | [Molecular Weight]
1563.76 |
| Chemical Properties | Back Directory | [density ]
1.57±0.1 g/cm3(Predicted) | [storage temp. ]
−20°C
| [form ]
solid
| [pka]
4.07±0.10(Predicted) | [Water Solubility ]
Soluble to 1 mg/ml in water |
| Hazard Information | Back Directory | [Uses]
HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats[1][2][3]. | [in vivo]
The dose-effect curve of morphine for locomotor activity was shifted downwards in C57Bl/6 mice pretreated with HS014 and in A(y) mice. The dose-effect curve of morphine for antinociception is shifted two- and threefold to the left in C57Bl/6 mice pretreated with HS014 and in A(y) mice, respectively[2].
Pretreatment with HS014 blocks the effect of IL-1beta on food intake and respiratory exchange ratio (RER) at later time points (beyond 8 h post injection), as well as the hypoactivity and increases metabolic rate[4]. | [IC 50]
MC4R | [storage]
Desiccate at -20°C | [References]
[1] Schi?th HB,et al. Discovery of novel melanocortin4 receptor selective MSH analogues. Br J Pharmacol. 1998;124(1):75-82. DOI:10.1038/sj.bjp.0701804
[2] Ercil NE, et al. HS014, a selective melanocortin-4 (MC4) receptor antagonist, modulates the behavioral effects of morphine in mice. Psychopharmacology (Berl). 2005;180(2):279-285. DOI:10.1007/s00213-005-2166-x
[3] Kask A, et al. Selective antagonist for the melanocortin 4 receptor (HS014) increases food intake in free-feeding rats. Biochem Biophys Res Commun. 1998;245(1):90-93. DOI:10.1006/bbrc.1998.8389 |
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