SHU 9119

目录号: HY-P0227 纯度: 99.95%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

SHU 9119 是有效地人类黑皮素受体 3 和 4 (MC3/4R) 拮抗剂，同时也是 MC5R 的部分激动剂，对人类 MC3R, MC4R 和 MC5R 的 IC₅₀ 值分别为 0.23, 0.06 和 0.09 nM。

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Custom Peptide Synthesis

SHU 9119 Chemical Structure

CAS No. : 168482-23-3

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规格	价格	是否有货
1 mg	￥1100	In-stock
5 mg	￥4400	In-stock
10 mg	现货	询价
50 mg		询价
100 mg		询价

or 大包装询价

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Customer Review

MCE 顾客使用本产品发表的 3 篇科研文献

SHU 9119 相关产品

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查看 Melanocortin Receptor 亚型特异性产品:

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MC1R MC3R MC2R MC4R MC5R

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

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.

IC₅₀ & Target

MC3R

MC4R

MC5R

细胞效力
(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]

体内研究
(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].

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

分子量

1074.24

Formula

C₅₄H₇₁N₁₅O₉

CAS 号

168482-23-3

性状

固体

颜色

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)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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)

溶解性数据

细胞实验：

H₂O 中的溶解度 : 10 mg/mL (9.31 mM; 超声助溶)

配制储备液

浓度溶剂体积质量	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	---	---	---

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

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

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。

纯度 & 产品资料

纯度: 99.95%

选择批次：

Data Sheet (613 KB) SDS (252 KB)

COA (179 KB) LCMS (86 KB) 元素分析报告 (219 KB)

产品使用指南 (1538 KB)

参考文献

[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.
参考文献	[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.

参考文献

[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]

SHU 9119 相关分类

Metabolic Disease

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

SHU 9119

Customer Review

MCE 顾客使用本产品发表的 3 篇科研文献