ChemicalBook > CAS DataBase List > SHU-9119

SHU-9119

Product Name
SHU-9119
CAS No.
168482-23-3
Chemical Name
SHU-9119
Synonyms
SHU-9119;SHU9119，TFA;CHEMBL3422426;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
CBNumber
CB7675726
Molecular Formula
C54H71N15O9
Formula Weight
1074.24
MOL File
168482-23-3.mol
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SHU-9119 Property

Density 
1.43±0.1 g/cm3(Predicted)
storage temp. 
-20°C
solubility 
H2O : 20 mg/mL (18.62 mM; Need ultrasonic)
form 
Powder
pka
13.00±0.70(Predicted)
color 
White to off-white
Water Solubility 
Soluble to 0.20 mg/ml in water
Sequence
Ac-Nle-Asp-His-D-Nal-Arg-Trp-Lys-NH2(Chemical Bridge Asp2-Lys7)
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Safety

WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
24152
Product name
SHU9119 (trifluoroacetate salt)
Purity
≥95%
Packaging
500μg
Price
$77
Updated
2024/03/01
Cayman Chemical
Product number
24152
Product name
SHU9119 (trifluoroacetate salt)
Purity
≥95%
Packaging
1mg
Price
$121
Updated
2024/03/01
Tocris
Product number
3420
Product name
SHU9119
Packaging
1
Price
$151
Updated
2021/12/16
Usbiological
Product number
256659
Product name
SHU 9119
Packaging
1mg
Price
$389
Updated
2021/12/16
ChemScene
Product number
CS-6496
Product name
SHU9119
Purity
98.21%
Packaging
5mg
Price
$468
Updated
2021/12/16
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SHU-9119 Chemical Properties,Usage,Production

Description

SHU9119 is an agonist of melanocortin receptor 1 (MC1R) and antagonist of MC4R (IC50s = 1.2 and 2.9 nM, respectively, for displacement of melanocortin). It induces cAMP formation in HEK293 cells expressing human MC1R (EC50 = 1.11 nM), but inhibits cAMP formation in cells expressing human MC4R. In rats, SHU9119 (24 nmol, i.c.v. per day for seven days) increases food intake, body weight, fat mass, and lean mass, with concomitant increases in blood glucose, insulin, and leptin levels via disrupted melanocortin signaling. Similarly, mice treated with SHU9119 (5 nmol/day, i.c.v.) exhibit food intake-independent increases in body weight and fat mass consequent to MC4R inhibition and subsequent brown adipose tissue dysfunction.

Uses

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.

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].

IC 50

MC3R; MC4R; MC5R

storage

Store at -20°C

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. DOI:10.1016/j.peptides.2007.02.012
[2] Nogueiras R, et al. The central melanocortin system directly controls peripheral lipid metabolism. J Clin Invest. 2007 Nov;117(11):3475-88. DOI:10.1172/JCI31743
[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. DOI:10.1194/jlr.M045989

SHU-9119 Preparation Products And Raw materials

Raw materials

Preparation Products

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SHU-9119 Suppliers

China 88 France 1 Germany 1 Japan 1 Switzerland 1 United Kingdom 1 United States 15 Global 108
3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
Fax
86-21-50328109
Email
3bsc@sina.com
Country
China
ProdList
15838
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Alabiochem Tech.Co., Ltd.
Tel
512-58900862 400-0707518
Fax
0086-512-56765862
Email
sales@alabiochem.com
Country
China
ProdList
970
Advantage
59
GL Biochem (Shanghai) Ltd
Tel
21-61263452 13641803416
Fax
86-21-61263399
Email
ymbetter@glbiochem.com
Country
China
ProdList
9981
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64
Shanghai Hanhong Scientific Co.,Ltd.
Tel
021-54306202 13764082696
Email
info@hanhongsci.com
Country
China
ProdList
42934
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64
Chemsky（shanghai）International Co.,Ltd.
Tel
021-50135380
Email
shchemsky@sina.com
Country
China
ProdList
32321
Advantage
50
Cellmano Biotech Limited
Tel
0551-65326643 18156095617
Fax
0551-65326641
Email
info@cellmano.com
Country
China
ProdList
1010
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55
BOC Sciences
Tel
1-631-485-4226; 16314854226
Email
info@bocsci.com
Country
United States
ProdList
12952
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MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4861
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58
Sigma-Aldrich
Tel
021-61415566 800-8193336
Email
orderCN@merckgroup.com
Country
China
ProdList
51395
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Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
71826
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60

168482-23-3, SHU-9119Related Search:

ALPHA-MSH ALPHA-MSH SHU 9119, [125I]- SHU-9119 Melanotan II

  • SHU-9119
  • [N-ACETYL-NLE4,ASP5,D-2'-NAL7,LYS10]-ALPHA-MSH (4-10) AMIDE, ASP5-LYS10, CYCLIC LACTAM
  • AC-NLE-ASP-HIS-D-2-NAL-ARG-TRP-LYS-NH2
  • AC-NLE-ASP-HIS-D-2'-NAL-ARG-TRP-LYS-NH2, ASP5-LYS10, CYCLIC LACTAM
  • AC-NLE-ASP-HIS-D-2-NAL-H2N-LYS-TRP-ARG
  • AC-NLE-ASP-HIS-D-NAL(2)-ARG-TRP-LYS-NH2
  • (AC-NLE4,ASP5,D-2-NAL7,LYS10)-CYCLO-ALPHA-MSH (4-10) AMIDE
  • AC-[NLE4, ASP5, D-2-NAL7, LYS10]-CYCLO-ALPHA-MSH AMIDE (4-10)
  • (AC-NLE4,ASP5,D-ALA(2-NAPHTHYL)7,LYS10)-CYCLO-ALPHA-MSH (4-10) AMIDE
  • AC-NLE4-C[ASP5, D-NAL(2)7, LYS10]ALPHA-MSH (4-10)-NH2
  • AC-NLE-CYCLO(-ASP-HIS-D-2-NAL-ARG-TRP-LYS-NH2) TRIFLUOROACETATE SALT
  • AC-NLE-CYCLO[(BETA-D)-H-(D-2-NAL)-RW-(EPSILON-K)]-NH2
  • AC-NLE-CYCLO(BETA-ASP-HIS-D-2-NAL-ARG-TRP-EPSILON-LYS)-NH2
  • AC-NLE-CYCLO(-BETA-ASP-HIS-D-ALA(2-NAPHTHYL)-ARG-TRP-EPSILON-LYS-NH2)
  • [ACETYL-NLE4, ASP5, D-2-NAL7, LYS10]-ALPHA-MELANOCYTE STIMULATING HORMONE (4-10) AMIDE
  • [ACETYL-NLE4, ASP5, D-2-NAL7, LYS10]-ALPHA-MSH (4-10) AMIDE
  • (ACETYL-NLE4,ASP5,D-2-NAL7,LYS10)-CYCLO-ALPHA-MSH (4-10) AMIDE TRIFLUOROACETATE SALT
  • (Ac-Nle4,Asp5,D-Ala(2-naphthyl)7,Lys10)-cyclo-a-MSH (4-10) amide
  • Acetyl-[Nle4, Asp5, D-2-Nal7, Lys10]-cyclo-α-Melanocyte Stimulating Hormone Amide Fragment 4-10
  • Acetyl-(Nle4,Asp5,D-2-Nal7,Lys10)-cyclo-α-MSH (4-10) aMide SHU9119
  • Ac-Nle-Asp-His-D-Nal(2)-Arg-Trp-Lys-NH2 (AMide bond Asp5-Lys10)
  • Acetyl-(Nle4,Asp5,D-2-Nal7,Lys10)-cyclo-a-MSH (4-10) aMide
  • Ac-Nle-cyclo(-Asp-His-D-2-Nal-Arg-Trp-Lys-NH2)
  • Acetyl-(Nle4,Asp5,D-2-Nal7,Lys10)-cyclo-Alpha-MSH (4-10) amide
  • SHU9119 (trifluoroacetate salt)
  • L-Lysinamide, N-acetyl-L-norleucyl-L-α-aspartyl-L-histidyl-3-(2-naphthalenyl)-D-alanyl-L-arginyl-L-tryptophyl-, (2→7)-lactam
  • Acetyl-(Nle4,Asp5,D-2-Nal7,Lys10)-cyclo-α-MSH (4-10) amide trifluoroacetate salt
  • CHEMBL3422426
  • Acetyl-(Nle4,Asp5,D-2-Nal7,Lys10)-cyclo-α-MSH (4-10) amide
  • Acetyl-(Nle4,Asp5,D-2-Nal7,Lys10)-cyclo-α-MSH (4-10) amide, SHU9119
  • Acetyl-(Nle?,Asp?,D-2-Nal?,Lys1?)-cyclo-α-MSH (4-10) amide trifluoroacetate salt
  • Acetyl-(Nle?,Asp?,D-2-Nal?,Lys??)-cyclo-α-MSH (4-10) amide trifluoroacetate salt
  • SHU9119，TFA
  • (3R,6R,9S,12R,15R,23R)-12-((1H-Imidazol-5-yl)methyl)-3-((1H-indol-3-yl)methyl)-15-((R)-2-acetamidohexanamido)-6-(3-guanidinopropyl)-9-(naphthalen-2-ylmethyl)-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexaazacyclotricosane-23-carboxamide
  • SHU9119, Melanocortin 3 and 4 (MC3 and MC4) receptor antagonist
  • N-Acetyl-L-norleucyl-L-a-aspartyl-L-histidyl-3-(2-naphthalenyl)-D-alanyl-L-arginyl-L-tryptophyl-L-lysinamide-(2,7) -lactam
  • 168482-23-3
  • C54H71N15O9