Setmelanotide TFA
Based on 8 publication(s) in Google Scholar
Setmelanotide TFA (RM-493 TFA) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively.
For research use only. We do not sell to patients.
- Formula: C51H69F3N18O11S2
- Molecular Weight:1231.33
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Setmelanotide TFA
More- Sci Transl Med. 2025 Jan 15;17(781):eadr6459. [Abstract]
- J Exp Med. 2021 Jul 5;218(7):e20202484. [Abstract]
- Cell Rep. 2022 Nov 1;41(5):111579. [Abstract]
- J Med Chem. 2017 Nov 9;60(21):8716-8730. [Abstract]
- Mol Metab. 2024 Sep 10:102027. [Abstract]
- Front Immunol. 2019 Oct 4;10:2312. [Abstract]
- J Clin Endocrinol Metab. 2024 Sep 16;109(10):2452-2466. [Abstract]
- Charles University. 2019 Jun.
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In Vivo Efficacy Study
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
Biological Activity
EC50: 5.8 nM (hMC1R), 5.3 nM (hMC3R), 0.27 nM (hMC4R), 0.28 nM (rMC4R), 1600 nM (hMC5R)[1]
Ki:3.9 nM (hMC1R), 10 nM (hMC3R), 2.1 nM (hMC4R), 430 nM (hMC5R), 2.7 nM (rMC4R)[1]
Chemical Information
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Molecular Weight 1231.33
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Formula C51H69F3N18O11S2
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Synonyms
RM-493 TFA; BIM-22493 TFA; IRC-022493 TFA
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Sequence
Ac-Arg-Cys-{d-Ala}-His-{d-Phe}-Arg-Trp-Cys-NH2 (Disulfide bridge:Cys2-Cys8)
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Sequence Shortening
Ac-RC-{d-Ala}-H-{d-Phe}-RWC-NH2 (Disulfide bridge:Cys2-Cys8)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (8)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
2025 Jan 15;17(781):eadr6459. PMID: 39813316
Setmelanotide TFA purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Jan 15;17(781):eadr6459. [Abstract]
Setmelanotide (2 mg/kg; i.p.; once daily for 9 d) reduced body weights and food intake and improved glucose tolerance of HFD-fed OtpQ153R/+ mice, which quickly regained body weight after the treatment was discontinued.
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J Exp Med
The atypical antipsychotic risperidone targets hypothalamic melanocortin 4 receptors to cause weight gain. [Abstract]2021 Jul 5;218(7):e20202484. PMID: 33978701
Setmelanotide TFA purchased from MedChemExpress. Usage Cited in: J Exp Med. 2021 Jul 5;218(7):e20202484. [Abstract]
Setmelanotide (100 nM) blocked the risperidone-induced hyperpolarization of MC4RPVH neurons.
Setmelanotide TFA purchased from MedChemExpress. Usage Cited in: J Exp Med. 2021 Jul 5;218(7):e20202484. [Abstract]
A single dose of Setmelanotide (SET) (2 mg/kg; i.p.) suppressed fast-induced refeeding in Mc4rfl/fl mice.
Setmelanotide TFA purchased from MedChemExpress. Usage Cited in: J Exp Med. 2021 Jul 5;218(7):e20202484. [Abstract]
Infusion of Setmelanotide (SET) (2 mg/kg; once daily for 14 d) attenuated hyperphagia in C57BL/6 mice fed with risperidone.
Setmelanotide TFA purchased from MedChemExpress. Usage Cited in: J Exp Med. 2021 Jul 5;218(7):e20202484. [Abstract]
Setmelanotide (SET) (2 mg/kg; once daily for 14 d) caused accelerated glucose clearance of C57BL/6 mice fed with risperidone in a GTT.
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Cell Rep
Melanocortin-4 receptors activate sympathetic preganglionic neurons and elevate blood pressure via TRPV1. [Abstract]2022 Nov 1;41(5):111579. PMID: 36323255 -
J Med Chem
2017 Nov 9;60(21):8716-8730. PMID: 28972753 -
Mol Metab
Lead-in calorie restriction enhances the weight-lowering efficacy of incretin hormone-based pharmacotherapies in mice. [Abstract]2024 Sep 10:102027. PMID: 39265725 -
Front Immunol
Setmelanotide, a Novel, Selective Melanocortin Receptor-4 Agonist Exerts Anti-inflammatory Actions in Astrocytes and Promotes an Anti-inflammatory Macrophage Phenotype. [Abstract]2019 Oct 4;10:2312. PMID: 31636637 -
J Clin Endocrinol Metab
MC4R variants modulate α-MSH and setmelanotide induced cellular signaling at multiple levels. [Abstract]2024 Sep 16;109(10):2452-2466. PMID: 38567654 -
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)