Setmelanotide

Alias: RM-493 ;Imcivree; RM493; BIM 22493; IRC-022493; RM493; BIM22493; IRC 022493; RM 493; BIM-22493; IRC022493

Cat No.:V28769 Purity: ≥98%

COA Product Data Instructions for use SDS

Setmelanotide Chemical Structure CAS No.: 920014-72-8
Product category: Melanocortin Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of Setmelanotide:

Setmelanotide TFA

Official Supplier of:

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Setmelanotide (BIM-22493; RM-493; IRC-022493; Imcivree) is a novel, selective and peptidyl agonist of melanocortin 4 receptor (MC4R) that has been approved in 2020 for use as an anti-obesity medication for the treatment of genetic obesity. Melanocortin 4 receptor (MC4R) activation occurs at EC50s of 0.27 nM for rat MC4R and 0.28 nM for human MC4R, respectively.

Biological Activity I Assay Protocols (From Reference)

Targets	MC4R ( EC50 = 0.27 nM ); MC4R ( Ki = 2.1 nM )
References	[1]. Analysis of the therapeutic functions of\nnovel melanocortin receptor agonists in MC3R- and MC4R-deficient\nC57BL/6J mice. Peptides. 2009 Oct;30(10):1892-900 [2]. Chronic treatment with a melanocortin-4\nreceptor agonist causes weight loss, reduces insulin resistance, and\nimproves cardiovascular function in diet-induced obese rhesus macaques.\nDiabetes. 2013 Feb;62(2):490-7. [3]. Melanocortin-4 receptor modulators for the treatment of obesity: a\npatent analysis (2008-2014). Pharm Pat Anal. 2015;4(2):95-107.

Targets

MC4R ( EC50 = 0.27 nM ); MC4R ( Ki = 2.1 nM )

References

[1]. Analysis of the therapeutic functions of\nnovel melanocortin receptor agonists in MC3R- and MC4R-deficient\nC57BL/6J mice. Peptides. 2009 Oct;30(10):1892-900

[2]. Chronic treatment with a melanocortin-4\nreceptor agonist causes weight loss, reduces insulin resistance, and\nimproves cardiovascular function in diet-induced obese rhesus macaques.\nDiabetes. 2013 Feb;62(2):490-7.

[3]. Melanocortin-4 receptor modulators for the treatment of obesity: a\npatent analysis (2008-2014). Pharm Pat Anal. 2015;4(2):95-107.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C₄₉H₆₈N₁₈O₉S₂
Molecular Weight	1117.31
Exact Mass	1116.49
CAS #	920014-72-8
Related CAS #	1301120-74-0 (pamoate); 920014-72-8 (free); 1504602-49-6 (acetate)
SMILES	C[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@@H](C(=O)N1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)C)C(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5
InChi Key	HDHDTKMUACZDAA-PHNIDTBTSA-N
InChi Code	InChI=1S/C49H68N18O9S2/c1-26-41(70)63-37(20-30-22-55-25-59-30)46(75)64-35(18-28-10-4-3-5-11-28)44(73)62-34(15-9-17-57-49(53)54)43(72)65-36(19-29-21-58-32-13-7-6-12-31(29)32)45(74)66-38(40(50)69)23-77-78-24-39(47(76)60-26)67-42(71)33(61-27(2)68)14-8-16-56-48(51)52/h3-7,10-13,21-22,25-26,33-39,58H,8-9,14-20,23-24H2,1-2H3,(H2,50,69)(H,55,59)(H,60,76)(H,61,68)(H,62,73)(H,63,70)(H,64,75)(H,65,72)(H,66,74)(H,67,71)(H4,51,52,56)(H4,53,54,57)/t26-,33+,34+,35-,36+,37+,38+,39+/m1/s1
Chemical Name	(4R,7S,10S,13R,16S,19R,22R)-22-[[(2S)-2-acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-13-benzyl-10-[3-(diaminomethylideneamino)propyl]-16-(1H-imidazol-5-ylmethyl)-7-(1H-indol-3-ylmethyl)-19-methyl-6,9,12,15,18,21-hexaoxo-1,2-dithia-5,8,11,14,17,20-hexazacyclotricosane-4-carboxamide
Synonyms	RM-493 ;Imcivree; RM493; BIM 22493; IRC-022493; RM493; BIM22493; IRC 022493; RM 493; BIM-22493; IRC022493
Storage	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)	DMSO: ~100 mg/mL (~89.5 mM) Water: ~100 mg/mL Ethanol: ~100 mg/mL
Solubility (In Vivo)	5%DMSO + 40%PEG300 + 5%Tween 80 + 50%ddH2O: 5.0mg/ml (4.48mM) (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	0.8950 mL	4.4750 mL	8.9501 mL
	5 mM	0.1790 mL	0.8950 mL	1.7900 mL
	10 mM	0.0895 mL	0.4475 mL	0.8950 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

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Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04963231	Active Recruiting	Drug: Setmelanotide Drug: Placebo	Genetic Obesity	Rhythm Pharmaceuticals, Inc.	November 30, 2021	Phase 2
NCT05093634	Recruiting	Drug: Setmelanotide Drug: Placebo	Obesity Genetic Obesity	Rhythm Pharmaceuticals, Inc.	December 10, 2021	Phase 3
NCT04725240	Completed	Drug: Setmelanotide	Hypothalamic Obesity	Rhythm Pharmaceuticals, Inc.	June 7, 2021	Phase 2
NCT04966741	Completed	Drug: Setmelanotide	Bardet-Biedl Syndrome POMC Deficiency Obesity	Rhythm Pharmaceuticals, Inc.	February 16, 2022	Phase 3
NCT03746522	Completed	Drug: Setmelanotide Drug: Placebo	Bardet Biedl Syndrome (BBS) Alström Syndrome (AS)	Rhythm Pharmaceuticals, Inc.	November 23, 2018	Phase 3

Biological Data

Response of melanocortin receptor knockout and diet-induced obese mice to BIM-22493 treatment. Peptides . 2009 Oct;30(10):1892-900.
BIM-22493 significantly improves hepatic steatosis in diet-induced obese mice. Peptides . 2009 Oct;30(10):1892-900.
BIM-22493 treatment reduces food intake, body weight, and core body temperature and increases activity and energy expenditure in obese NHP. Diabetes . 2013 Feb;62(2):490-7.
BIM-22493 treatment reduced fat mass, leptin levels, lean mass, and triglycerides in obese NHP. Diabetes . 2013 Feb;62(2):490-7.
BIM-22493 ameliorates insulin resistance in obese NHP. Diabetes . 2013 Feb;62(2):490-7.