HS 014 TFA

Modify Date: 2024-01-02 09:39:51

HS 014 TFA Structure
HS 014 TFA structure
Common Name HS 014 TFA
CAS Number 207678-81-7 Molecular Weight 1563.760
Density 1.6±0.1 g/cm3 Boiling Point N/A
Molecular Formula C71H94N20O17S2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of HS 014 TFA


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].

 Names

Name hs 014
Synonym More Synonyms

 HS 014 TFA 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
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

 Synonyms

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
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