207678-81-7
Chemical Structure
HS014
- CAS No.: 207678-81-7
- Formula:C71H94N20O17S2
- Molecular Weight:1563.76
IUPAC Name: (S)-3-((S)-2-((S)-1-(((4R,10S,13S,16R,19S,22S,25R)-19-((1H-imidazol-5-yl)methyl)-10-((1H-indol-3-yl)methyl)-25-acetamido-22-(2-carboxyethyl)-13-(3-guanidinopropyl)-16-(naphthalen-2-ylmethyl)-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptaa
InChIKey: BRGDPINZISNYJL-VMAVSDBDSA-N
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
Biological Activity: 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].
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HS014 | 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. | |||||||||||||||||||||
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- [1]. Schiöth HB,et al. Discovery of novel melanocortin4 receptor selective MSH analogues. Br J Pharmacol. 1998;124(1):75-82. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
Keywords