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SHU 9119 acetate

Catalog No. T16879L CAS 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, CAS T16879L

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Purity: 98%

Biological Description

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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	hMC5R:0.09 nM, hMC4R:0.06 nM, hMC3R:0.23 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
CAS No.	T16879L

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 55 mg/ml (48.49 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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 Products

Related compounds with same targets

HS 014 acetate(207678-81-7 free base) HS024 [D-Trp8]-γ-MSH acetate(321351-81-9 free base) Melanotan (MT)-II ACTH 11-24 acetate(4237-93-8 free base) α-MSH Adrenocorticotropic Hormone (ACTH) (4-10), human Bremelanotide Acetate

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Keywords

SHU 9119 acetate T16879L G蛋白偶联受体神经科学 Melanocortin Receptor SHU 9119 acetate (168482-23-3 free base) Inhibitor inhibitor inhibit

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