Product Name :
SHU 9119
Description:
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.
CAS:
168482-23-3
Molecular Weight:
1074.24
Formula:
C54H71N15O9
Chemical Name:
(3S,6S,9R,12S,15S,23S)-6-{3-[(diaminomethylidene)amino]propyl}-15-[(2S)-2-acetamidohexanamido]-12-[(1H-imidazol-5-yl)methyl]-3-[(1H-indol-3-yl)methyl]-9-[(naphthalen-2-yl)methyl]-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexaazacyclotricosane-23-carboxamide
Smiles :
CC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@H](CC2=CNC3=CC=CC=C23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC2=CC3=CC=CC=C3C=C2)NC(=O)[C@H](CC2=CN=CN2)NC1=O)C(N)=O
InChiKey:
GGYWLZFXFKFWKL-XOJVSUSESA-N
InChi :
InChI=1S/C54H71N15O9/c1-3-4-15-40(63-31(2)70)48(73)69-45-27-46(71)59-21-10-9-17-39(47(55)72)64-51(76)43(25-35-28-61-38-16-8-7-14-37(35)38)67-49(74)41(18-11-22-60-54(56)57)65-50(75)42(24-32-19-20-33-12-5-6-13-34(33)23-32)66-52(77)44(68-53(45)78)26-36-29-58-30-62-36/h5-8,12-14,16,19-20,23,28-30,39-45,61H,3-4,9-11,15,17-18,21-22,24-27H2,1-2H3,(H2,55,72)(H,58,62)(H,59,71)(H,63,70)(H,64,76)(H,65,75)(H,66,77)(H,67,74)(H,68,78)(H,69,73)(H4,56,57,60)/t39-,40-,41-,42+,43-,44-,45-/m0/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.{{GLP-1 receptor agonist 2} site|{GLP-1 receptor agonist 2} GPCR/G Protein|{GLP-1 receptor agonist 2} Purity & Documentation|{GLP-1 receptor agonist 2} References|{GLP-1 receptor agonist 2} manufacturer|{GLP-1 receptor agonist 2} Cancer}
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.{{HBC} MedChemExpress|{HBC} Cell Cycle/DNA Damage|{HBC} Technical Information|{HBC} Description|{HBC} manufacturer|{HBC} Autophagy}
Additional information:
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.|Product information|CAS Number: 168482-23-3|Molecular Weight: 1074.24|Formula: C54H71N15O9|Chemical Name: (3S,6S,9R,12S,15S,23S)-6-{3-[(diaminomethylidene)amino]propyl}-15-[(2S)-2-acetamidohexanamido]-12-[(1H-imidazol-5-yl)methyl]-3-[(1H-indol-3-yl)methyl]-9-[(naphthalen-2-yl)methyl]-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexaazacyclotricosane-23-carboxamide|Smiles: CC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@H](CC2=CNC3=CC=CC=C23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC2=CC3=CC=CC=C3C=C2)NC(=O)[C@H](CC2=CN=CN2)NC1=O)C(N)=O|InChiKey: GGYWLZFXFKFWKL-XOJVSUSESA-N|InChi: InChI=1S/C54H71N15O9/c1-3-4-15-40(63-31(2)70)48(73)69-45-27-46(71)59-21-10-9-17-39(47(55)72)64-51(76)43(25-35-28-61-38-16-8-7-14-37(35)38)67-49(74)41(18-11-22-60-54(56)57)65-50(75)42(24-32-19-20-33-12-5-6-13-34(33)23-32)66-52(77)44(68-53(45)78)26-36-29-58-30-62-36/h5-8,12-14,16,19-20,23,28-30,39-45,61H,3-4,9-11,15,17-18,21-22,24-27H2,1-2H3,(H2,55,72)(H,58,62)(H,59,71)(H,63,70)(H,64,76)(H,65,75)(H,66,77)(H,67,74)(H,68,78)(H,69,73)(H4,56,57,60)/t39-,40-,41-,42+,43-,44-,45-/m0/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: H2O : 20 mg/mL (18.PMID:23539298 62 mM; Need ultrasonic).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|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.|Products are for research use only. Not for human use.|