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SHU 9119 acetate

Catalog No. T16879L
Synonyms: SHU 9119 acetate (168482-23-3 free base)

SHU 9119 acetate is a well-known antagonist of human melanocortin 3 and 4 (hMC3R, hMC4R) receptors and a partial hMC5R agonist. The IC50 values of human MC3R, MC4R and MC5R is 0.23, 0.06, and 0.09 nM respectively.

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SHU 9119 acetate Chemical Structure
SHU 9119 acetate, CAS N/A
Pack Size Availability Price/USD Quantity
1 mg In stock $ 89.00
5 mg In stock $ 383.00
10 mg In stock $ 575.00
25 mg In stock $ 923.00
50 mg In stock $ 1,260.00
1 mL * 10 mM (in DMSO) In stock $ 647.00
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Purity: 99.8%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SHU 9119 acetate is a well-known antagonist of human melanocortin 3 and 4 (hMC3R, hMC4R) receptors and a partial hMC5R agonist. The IC50 values of human MC3R, MC4R and MC5R is 0.23, 0.06, and 0.09 nM respectively.
Targets&IC50 MC5R (human):0.09 nM, MC3R (human):0.23 nM, MC4R (human):0.06 nM
In vivo Compared with control, blocking CNS-Mcr by chronic intracerebroventricular infusion of SHU9119 (24 nmol/d for 7 days) increases food intake in ad libitum-fed rats. Weight gain of SHU9119 treated rats is significantly higher than control. SHU9119 treatment effectively 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. SHU9119 increases food intake (+30%) and body fat (+50%) and decreases EE by reduction in fat oxidation (?42%). Furthermore, 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.
Synonyms SHU 9119 acetate (168482-23-3 free base)
Molecular Weight 1134.29
Formula C56H75N15O11

Storage

keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/ml (48.49 mM)

TargetMolReferences and Literature

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 Peptides. 2007 Jun;28(6):1191-6. 2. Nogueiras R, et al. The central melanocortin system directly controls peripheral lipid metabolism. J Clin Invest. 2007 Nov;117(11):3475-88. 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.

Related compound libraries

This product is contained In the following compound libraries:
Membrane Protein-targeted Compound Library GPCR Compound Library Inhibitor Library Bioactive Compound Library NO PAINS Compound Library Bioactive Compounds Library Max Anti-Obesity Compound Library

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Keywords

SHU 9119 acetate GPCR/G Protein Neuroscience Melanocortin Receptor 168482-23-3 free base SHU 9119 Acetate SHU-9119 Acetate 168482-23-3 SHU 9119 acetate (168482-23-3 free base) SHU9119 Acetate inhibitor inhibit

 

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