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Setmelanotide Acetate(920014-72-8 free base)

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Catalog No. T12882LCas No. 2759937-80-7
Alias RM-493 Acetate, IRC-022493 Acetate, BIM-22493 Acetate

Setmelanotide Acetate(920014-72-8 free base) (RM-493 Acetate) is a selective agonist of melanocortin 4 receptor (MC4R)(human and rat MC4R with EC50s of 0.27 nM and 0.28 nM, respectively).

Setmelanotide Acetate(920014-72-8 free base)
Other Forms of Setmelanotide Acetate(920014-72-8 free base):
SetmelanotideT12882920014-72-8
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Setmelanotide Acetate(920014-72-8 free base)

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Purity: 99.71%
Catalog No. T12882LAlias RM-493 Acetate, IRC-022493 Acetate, BIM-22493 AcetateCas No. 2759937-80-7
Setmelanotide Acetate(920014-72-8 free base) (RM-493 Acetate) is a selective agonist of melanocortin 4 receptor (MC4R)(human and rat MC4R with EC50s of 0.27 nM and 0.28 nM, respectively).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$133In StockIn Stock
5 mg$302In StockIn Stock
10 mg$453In StockIn Stock
25 mg$748-In Stock
50 mg$1,050-In Stock
100 mg$1,420InquiryInquiry
1 mL x 10 mM (in DMSO)$585In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information

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Purity:99.71%
Appearance:Solid
Color:White
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COA LCMS HNMR

Product Introduction

Bioactivity
Description
Setmelanotide Acetate(920014-72-8 free base) (RM-493 Acetate) is a selective agonist of melanocortin 4 receptor (MC4R)(human and rat MC4R with EC50s of 0.27 nM and 0.28 nM, respectively).
Targets&IC50
MC4R (human): 0.27 nM (EC50), MC4R (human): 2.1 nM (ki), MC5R (human): 1600 nM (EC50), MC5R (human): 430 nM (ki), MC3R (human): 10 nM (ki), MC3R (human): 5.3nM (EC50), MC4R (rat): 2.7 nM (ki), MC4R (rat):0.28 Nm (EC50), MC1R (human):3.9 nM (ki), MC1R (human):5.8 nM (EC50)
In vitro
Melanocortin receptor agonists act in the brain to regulate food intake and body weight and, independently of these actions, affect insulin sensitivity. Setmelanotide exhibits agonist activity to human and rat MC4R(human and rat MC4R with Kis of 2.1 and 2.7 nM and EC50s of 0.27 and 0.28 nM, respectively)[1].
In vivo
Inhibition of refeeding after an overnight fast by BIM-22493 is dependent on functional MC4R.glucose homeostasis acutely improved by BIM-22493. BIM-22493(Lepob/Lepob mice) exhibits significantly improved glucose clearance when compared to controls. Chronic BIM-22493 treatment was associated with significantly lower levels of serum insulin, glucose and HOMA-IR values, suggesting an improvement in insulin sensitivity[1]. Treatment with setmelanotide results in transient decreases in food intake (35%), with persistent weight loss over 8 weeks of treatment (13.5%) in a diet-induced obese nonhuman primate model[2].
SynonymsRM-493 Acetate, IRC-022493 Acetate, BIM-22493 Acetate
Chemical Properties
Molecular Weight1177.35
FormulaC51H72N18O11S2
Cas No.2759937-80-7
SmilesO=C([C@@H](NC([C@H](NC([C@@H](NC([C@H](NC([C@H](CSSC[C@H](NC1=O)C(N)=O)NC([C@@H](NC(C)=O)CCCNC(N)=N)=O)=O)C)=O)CC2=CN=CN2)=O)CC3=CC=CC=C3)=O)CCCNC(N)=N)N[C@H]1CC4=CNC5=CC=CC=C45.CC(O)=O
Relative Density.no data available
SequenceAc-Arg-Cys(1)-D-Ala-His-D-Phe-Arg-Trp-Cys(1)-NH2
Sequence ShortRCAHFRWC
Storage & Solubility Information
Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 22.5 mg/mL (19.11 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (1.7 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM0.8494 mL4.2468 mL8.4937 mL42.4683 mL
5 mM0.1699 mL0.8494 mL1.6987 mL8.4937 mL
10 mM0.0849 mL0.4247 mL0.8494 mL4.2468 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
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Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

Setmelanotide Acetate(920014-72-8 free base)Setmelanotide Acetate(920014728 free base)Setmelanotide Acetate(920014 72 8 free base)rMC4RRM493 AcetateRM 493 AcetateMelanocortinReceptorMelanocortin ReceptorIRC022493 AcetateIRC 022493 AcetatehMC5RhMC4RhMC3RhMC1RBIM22493 AcetateBIM 22493 Acetate
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