SHU-9119
SHU-9119 Basic information
- Product Name:
- SHU-9119
- Synonyms:
-
- SHU-9119
- [N-ACETYL-NLE4,ASP5,D-2'-NAL7,LYS10]-ALPHA-MSH (4-10) AMIDE, ASP5-LYS10, CYCLIC LACTAM
- AC-NLE-ASP-HIS-D-2-NAL-ARG-TRP-LYS-NH2
- AC-NLE-ASP-HIS-D-2'-NAL-ARG-TRP-LYS-NH2, ASP5-LYS10, CYCLIC LACTAM
- AC-NLE-ASP-HIS-D-2-NAL-H2N-LYS-TRP-ARG
- AC-NLE-ASP-HIS-D-NAL(2)-ARG-TRP-LYS-NH2
- (AC-NLE4,ASP5,D-2-NAL7,LYS10)-CYCLO-ALPHA-MSH (4-10) AMIDE
- AC-[NLE4, ASP5, D-2-NAL7, LYS10]-CYCLO-ALPHA-MSH AMIDE (4-10)
- CAS:
- 168482-23-3
- MF:
- C54H71N15O9
- MW:
- 1074.24
- Mol File:
- 168482-23-3.mol
SHU-9119 Chemical Properties
- Density
- 1.43±0.1 g/cm3(Predicted)
- storage temp.
- -20°C
- solubility
- H2O : 20 mg/mL (18.62 mM; Need ultrasonic)
- form
- Powder
- pka
- 13.00±0.70(Predicted)
- color
- White to off-white
- Water Solubility
- Soluble to 0.20 mg/ml in water
- Sequence
- Ac-Nle-Asp-His-D-Nal-Arg-Trp-Lys-NH2(Chemical Bridge Asp2-Lys7)
SHU-9119 Usage And Synthesis
Description
SHU9119 is an agonist of melanocortin receptor 1 (MC1R) and antagonist of MC4R (IC50s = 1.2 and 2.9 nM, respectively, for displacement of melanocortin). It induces cAMP formation in HEK293 cells expressing human MC1R (EC50 = 1.11 nM), but inhibits cAMP formation in cells expressing human MC4R. In rats, SHU9119 (24 nmol, i.c.v. per day for seven days) increases food intake, body weight, fat mass, and lean mass, with concomitant increases in blood glucose, insulin, and leptin levels via disrupted melanocortin signaling. Similarly, mice treated with SHU9119 (5 nmol/day, i.c.v.) exhibit food intake-independent increases in body weight and fat mass consequent to MC4R inhibition and subsequent brown adipose tissue dysfunction.
Uses
SHU 9119 is a potent human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist; with IC50 values of 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively.
in vivo
Blockade of CNS-Mcr via chronic intracerebroventricular infusion of SHU9119 (24 nmol/d for 7 days) increases food intake in ad libitum-fed rats compared with control. Weight gain of SHU9119 treated rats is significantly higher than control. SHU9119 treatment potently increases metabolic efficiency. SHU9119 markedly increases mRNA levels of genes promoting lipogenesis and TAG storage in adipocytes, including stearoyl-CoA desaturase-1, lipoprotein lipase, acetyl-CoA carboxylase α, and fatty acid synthase[2]. SHU9119 increases food intake (+30%) and body fat (+50%) and decreases EE by reduction in fat oxidation (?42%). In addition, SHU9119 impairs the uptake of VLDL-TG by BAT. In line with this, SHU9119 decreases uncoupling protein-1 levels in BAT (?60%) and induces large intracellular lipid droplets, indicative of severely disturbed BAT activity[3].
IC 50
MC3R; MC4R; MC5R
storage
Store at -20°C
References
[1] Grieco P, et al. Further structure-activity studies of lactam derivatives of MT-II and SHU-9119: their activity and selectivity at human melanocortin receptors 3, 4, and 5. Peptides. 2007 Jun;28(6):1191-6. DOI:10.1016/j.peptides.2007.02.012
[2] Nogueiras R, et al. The central melanocortin system directly controls peripheral lipid metabolism. J Clin Invest. 2007 Nov;117(11):3475-88. DOI:10.1172/JCI31743
[3] Kooijman S, et al. Inhibition of the central melanocortin system decreases brown adipose tissue activity. J Lipid Res. 2014 Oct;55(10):2022-32. DOI:10.1194/jlr.M045989
SHU-9119Supplier
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