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Setmelanotide

SKU: orb1708548

Description

Setmelanotide is a potent and selective MC4R agonist (EC50 ~0.27 nM) used to investigate obesity, metabolic disorders, and neuroendocrine pathways. Its applications include in vitro studies of receptor signaling and inflammation, as well as in vivo research on energy homeostasis, drug-induced weight gain, and blood pressure modulation.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number920014-72-8
MW1117.31
Purity99.93%
FormulaC49H68N18O9S2
SMILESC(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC=CC=C4)NC(=O)[C@H](CC5=CN=CN5)NC(=O)[C@@H](C)NC(=O)[C@@H](NC([C@H](CCCNC(=N)N)NC(C)=O)=O)CSSC[C@@H](C(N)=O)NC3=O
TargetMelanocortin Receptor
Solubility10% DMSO+40% PEG300+5% Tween-80+45% Saline:3.3 mg/mL (2.95 mM);DMSO:100 mg/mL (89.5 mM);H2O:50 mg/mL (44.75 mM)

Bioactivity

Target IC50
MC5R (human):1600 nM (EC50)|MC5R (human):430 nM (ki)|MC4R (rat):0.28 Nm (EC50)|MC4R (rat):2.7 nM (ki)|MC3R (human):5.3nM (EC50)|MC3R (human):10 nM (ki)|MC4R (human):0.27 nM (EC50)|MC4R (human):2.1 nM (ki)|MC1R (human):3.9 nM (ki)|MC1R (human):5.8 nM (EC50)
In Vivo
The inhibitory effect of Setmelanotide on refeeding behavior in mice fasted overnight is receptor-specific, which is dependent on the mediation of functional MC4R but independent of MC3R. Compared with the control group, Lep⁰ᵇ/Lep⁰ᵇ mice treated with BIM-22493 exhibited significantly enhanced glucose clearance capacity. Moreover, chronic administration of BIM-22493 was associated with marked reductions in blood glucose levels and HOMA-IR index in mice. In the diet-induced obese non-human primate model, an 8-week treatment with setmelanotide (13.5%) resulted in a transient 35% decrease in food intake and a concomitant sustained reduction in body weight.
In Vitro
Melanocortin receptor agonists act in the brain to regulate food intake and body weight, and also exert additional independent effects. Setmelanotide exhibits agonistic activity toward the melanocortin 4 receptor (MC4R) in both humans and rats, with a Ki value of 2.1 nM and an EC₅₀ value of 0.27 nM for human MC4R, and a Ki value of 2.7 nM and an EC₅₀ value of 0.28 nM for rat MC4R.

Storage & Handling

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.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

BIM 22493, BIM22493, BIM-22493, IRC 022493, IRC022493, IRC-022493, hMC1R, hMC3R, hMC4R, hMC5R, MelanocortinReceptor, Melanocortin Receptor, RM 493, rMC4R, RM493, RM-493, Setmelanotide

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Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Key Properties

No computed properties available.

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Setmelanotide (orb1708548)

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% DMSO +
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% Tween 80 +
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Available Sizes

Select a size below

1 mg
¥ 1,170.00
5 mg
¥ 2,080.00
10 mg
¥ 2,990.00
1 ml x 10 mM (in DMSO)
¥ 3,380.00
25 mg
¥ 4,420.00
50 mg
¥ 6,370.00
100 mg
¥ 8,970.00
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