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HS 014 TFA

Names

[ CAS No. ]:
207678-81-7

[ Name ]:
HS 014 TFA

[Synonym ]:
mc4receptor antagonist
1-{[(4R,10S,13S,16R,19S,22S,25R)-25-Acetamido-13-(3-carbamimidamidopropyl)-22-(2-carboxyethyl)-19-(1H-imidazol-4-ylmethyl)-10-(1H-indol-3-ylmethyl)-16-(2-naphthylmethyl)-6,9,12,15,18,21,24-heptaoxo-1, ;2-dithia-5,8,11,14,17,20,23-heptaazacyclohexacosan-4-yl]carbonyl}-L-prolyl-L-prolyl-L-lysyl-L-α-asparagine
L-α-Asparagine, 1-[[(4R,10S,13S,16R,19S,22S,25R)-25-(acetylamino)-13-[3-[(aminoiminomethyl)amino]propyl]-22-(2-carboxyethyl)-19-(1H-imidazol-4-ylmethyl)-10-(1H-indol-3-ylmethyl)-16-(2-naphthalenyl methyl)-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptaazacyclohexacos-4-yl]carbonyl]-L-prolyl-L-prolyl-L-lysyl-
HS014
AC-CYS-GLU-HIS-D-2-NAL-ARG-TRP-GLY-CYS-PRO-PRO-LYS-ASP-NH2
M.W. 1563.77 C71H94N20O17S2

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> Melanocortin Receptor

[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].

[References]

[1]. Schiöth HB,et al. Discovery of novel melanocortin4 receptor selective MSH analogues. Br J Pharmacol. 1998;124(1):75-82.

[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.

[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.

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Molecular Formula ]:
C71H94N20O17S2

[ Molecular Weight ]:
1563.760

[ Exact Mass ]:
1562.654663

[ PSA ]:
632.30000

[ LogP ]:
-3.97

[ Index of Refraction ]:
1.730

Safety Information

[ Safety Phrases ]:
22-24/25

[ WGK Germany ]:
3

Related Compounds