Size | Price | Stock | Qty |
---|---|---|---|
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
Other Sizes |
|
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.
Targets |
MC4R ( EC50 = 0.27 nM ); MC4R ( Ki = 2.1 nM )
|
---|---|
References |
[3]. Melanocortin-4 receptor modulators for the treatment of obesity: a\npatent analysis (2008-2014). Pharm Pat Anal. 2015;4(2):95-107. |
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)
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
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
|
HS Tariff Code |
2934.99.9001
|
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 (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.
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.
(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.
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 |
Response of melanocortin receptor knockout and diet-induced obese mice to BIM-22493 treatment. Peptides . 2009 Oct;30(10):1892-900. td> |
BIM-22493 significantly improves hepatic steatosis in diet-induced obese mice. Peptides . 2009 Oct;30(10):1892-900. td> |
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. td> |
BIM-22493 treatment reduced fat mass, leptin levels, lean mass, and triglycerides in obese NHP. Diabetes . 2013 Feb;62(2):490-7. td> |
BIM-22493 ameliorates insulin resistance in obese NHP. Diabetes . 2013 Feb;62(2):490-7. td> |