SHU 9119

Name: SHU 9119
Brand: MedChemExpress
SKU: HY-P0227
Rating: 5.0 (3 reviews)

Cat. No.: HY-P0227 Purity: 99.95%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

SHU 9119 Chemical Structure

CAS No. : 168482-23-3

Size	Price	Stock	Quantity
1 mg	USD 119	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 515	In-stock	Estimated Time of Arrival: December 31
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50 mg		Get quote

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Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE SHU 9119

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View All Melanocortin Receptor Isoform Specific Products:

View All Isoforms

MC1R MC3R MC2R MC4R MC5R

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

MC3R

MC4R

MC5R

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	> 100000 nM Compound: SHU9119	Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay	[PMID: 25699138]
HEK293	EC₅₀	0.64 nM Compound: SHU9119	Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay	[PMID: 25898270]
HEK293	EC₅₀	0.67 nM Compound: SHU9119	Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay	[PMID: 25699138]
HEK293	EC₅₀	2.31 nM Compound: SHU9119	Agonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassay Agonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassay	[PMID: 25898270]
HEK293	EC₅₀	2.4 nM Compound: SHU9119	Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay	[PMID: 25699138]
HEK293	EC₅₀	3 nM Compound: SHU9119	Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay	[PMID: 25699138]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

1074.24

Formula

C₅₄H₇₁N₁₅O₉

CAS No.

168482-23-3

Appearance

Solid

Color

White to off-white

Sequence

Ac-{Nle}-Asp-His-{d-Nal}-Arg-Trp-Lys-NH2 (Lactam bridge: Asp2-Lys7)

Sequence Shortening

Ac-{Nle}-DH-{d-Nal}-RWK-NH2 (Lactam bridge: Asp2-Lys7)

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture and light

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

H₂O : 10 mg/mL (9.31 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.9309 mL	4.6545 mL	9.3089 mL
5 mM	0.1862 mL	0.9309 mL	1.8618 mL
10 mM	---	---	---

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (283 KB) SDS (252 KB)

COA (257 KB) LCMS (86 KB) Elemental Analysis Report (116 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

[2]. Nogueiras R, et al. The central melanocortin system directly controls peripheral lipid metabolism. J Clin Invest. 2007 Nov;117(11):3475-88. [Content Brief]

[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. [Content Brief]

Animal Administration
^[2]^[3]

Rats: SHU9119 is prepared in saline. SHU9119 is infused i.c.v. at a concentration of 24 nM and MTII at a concentration of 1 nM per day for 2 or 7 days. To differentiate between SHU9119 effects per se from those related to increased food intake, we prevent overeating in a group of SHU9119-treated rats by pair-feeding, so that they are given the same amount of food as consumed by a control group (SHU9119-pf). The pair-feeding regimen consists in giving one-third of the daily food amount in the morning and the remaining two-thirds just before onset of darkness. Thus, most of the experiments include 5 groups of animals: an ad libitum–fed control group infused with i.c.v. saline; 2 i.c.v. SHU9119-infused groups: SHU9119–ad lib and SHU9119-pf; an MTII-infused group; and a saline-pf group^[2].

Mice: SHU9119 is prepared in artificial cerebrospinal fluid. After 4 weeks of run-in diet, mice are randomized into groups that received icv administration of artificial cerebrospinal fluid (vehicle) or SHU9119 (5 nmol/day) in vehicle during 14-17 days. The effect of SHU9119 on BAT activity independent of food intake is also investigated by using an additional SHU9119-treated group that is pair-fed (SHU9119-pf) to the vehicle-treated group. To achieve pair-feeding, food intake of the ad libitum-fed mice is monitored daily, and pair-fed mice receive surgery 1 day behind the control mice. The pair-feeding regimen consisted of giving the mice the average daily consumed food amount by the control mice, just before onset of darkness^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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. [Content Brief]

[2]. Nogueiras R, et al. The central melanocortin system directly controls peripheral lipid metabolism. J Clin Invest. 2007 Nov;117(11):3475-88. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	0.9309 mL	4.6545 mL	9.3089 mL	23.2723 mL
H₂O	5 mM	0.1862 mL	0.9309 mL	1.8618 mL	4.6545 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

SHU 9119 Related Classifications

Metabolic Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SHU 9119168482-23-3SHU9119SHU-9119Melanocortin ReceptorMC ReceptorInhibitorinhibitorinhibit

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SHU 9119

Customer Review

SHU 9119 Related Antibodies

3 Publications Citing Use of MCE SHU 9119

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Melanocortin Receptor Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

SHU 9119 Related Classifications

Keywords:

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