SHU 9119|168482-23-3|-陌孚医药/Medlife

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SHU 9119

目录号: PC10950 纯度: ≥98%

CAS No. :168482-23-3

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中文名称

SHU 9119

中文别名

N-乙酰基-L-正亮氨酰-L-alpha-天冬氨酰-L-组氨酰-3-(2-萘基)-D-丙氨酰-L-精氨酰-L-色氨酰-L-赖氨酰胺(2→7)-内酰胺;SHU-9119;（3S，6S，9R，12S，15S，23S）-15-[（N-乙酰基-L-去甲酰基）氨基]-6-{3-[（二氨基甲基）氨基]丙基}-12-（1H-咪唑-5-基甲基）-3-（1H-吲哚-3-基甲基）-9-（2-萘基甲基）-2,5,8,11,14,17-六氧基-1,4,7,10,18-六氮杂环三甲酰胺-23-甲酰胺

英文名称

SHU 9119

英文别名

Acetyl-(Nle?00Asp?00D-2-Nal?00Lys??)-cyclo-α-MSH(4-10)amide;Acetyl-(Nle4,Asp5,D-2-Nal7,Lys10)-cyclo-α-MSH (4-10) amide;L-Lysinamide,N-acetyl-L-norleucyl-L-a-aspartyl-L-histidyl-3-(2-naphthalenyl)-D-alanyl-L-arginyl-L-tryptophyl-,(2®SHU 9119;SHU-9119;3-naphthalen-2-yl-D-alanyl-N5-(diaminomethylidene)-L-ornithyl-N-[(3S,6S,13E)-6-[(N-acetyl-L-norleucyl)amino]-3-(4H-imidazol-4-ylmethyl)-2,5,8,15-tetraoxo-1,4,9-triazacyclopentadec-13-en-14-yl]-3-(2,3-dihydro-1H-indol-3-yl)-L-alaninamide;Ac-Nle-cyclo[Asp-His-D-Nal(2')-Arg-Trp-Lys]-NH2;MBX36;MBX-36;XDHXRWK;SHU9119 (trifluoroacetate salt);AC-NLE-ASP-HIS-D-2-NAL-ARG-TRP-LYS-NH2;AC-NLE-ASP-HIS-D-2-NAL-H2N-LYS-TRP-ARG;AC-NLE-ASP-HIS-D-NAL(2)-ARG-TRP-LYS-NH2;Ac-Nle-cyclo(-Asp-His-D-2-Nal-Arg-Trp-Lys-NH2);AC-NLE4-C[ASP5, D-NAL(2)7, LYS10]ALPHA-MSH (4-10)-NH2;AC-NLE-CYCLO[(BETA-D)-H-(D-2-NAL)-RW-(EPSILON-K)]-NH2;(AC-NLE4,ASP5,D-2-NAL7,LYS10)-CYCLO-ALPHA-MSH (4-10) AMIDE;AC-NLE-CYCLO(BETA-ASP-HIS-D-2-NAL-ARG-TRP-EPSILON-LYS)-NH2;(9S,23R)-15-(2-Acetamidohexanoylamino)-6-[3-(diaminomethylideneamino)propyl]-12-(1H-imidazol-5-ylmet;,18-hexaazacyclotricosan-23-carboxamid;3,18-hexaazacyclotricosane-23-carboxamide;,18-hexaazacyclotricosane-23-carboxamide;enylmethyl)-2,5,8,11,14,17-hexaoxo-, (3S,6S,9R,12S,15S,23S)-;Acetyl-(Nle4,Asp5,D-2-Nal7,Lys10)-cyclo-??-MSH (4-10) amide;L-Lysinamide,N-acetyl-L-norleucyl-L-a-aspartyl-L-histidyl-3-(2-naphthalenyl)-D-alanyl-L-arginyl-L-tryptophyl-,(2®7)-lactam;(3S,6S,9R,12S,15S,23S)-15-[(N-Acetyl-L-norleucyl)amino]-6-{3-[(diaminomethylene)amino]propyl}-12-(1H

Cas No.

168482-23-3

分子式

C₅₄H₇₁N₁₅O₉

分子量

1074.24

包装储存

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)

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.

性状

Solid

IC50 & Target[1][2]

MC3R

MC4R

MC5R

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. 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.

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

运输条件

Room temperature or refrigerated transportation.

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)

SequenceShortening

Ac-{Nle}-cyclo[DHD-{Nal}-RWK]-NH2

Sequence

Ac-{Nle}-cyclo[Asp-His-D-{Nal}-Arg-Trp-Lys]-NH2

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. [Information]

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

[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. [Information]

溶解度数据

体外研究:

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

配制储备溶液

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	---	---	---

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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