HS 014

Pricing Availability   Qty
Cat.No. 1831 - HS 014 | Ac-Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys-Pro-Pro-Lys-Asp-NH2 (Disulfide bridge: 1 - 8) | CAS No. 207678-81-7
Description: Selective MC4 receptor antagonist
Datasheet
Citations (1)
Reviews
Literature

Biological Activity

Potent and selective melanocortin MC4 receptor antagonist (Ki values are 3.16, 108, 54.4 and 694 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively). Increases food intake in rats and nociception in mice following central administration in vivo. Also inhibits IL-1β-induced Fos expression in the paraventricular hypothalamus.

Technical Data

M. Wt 1563.77
Formula C71H94N20O17S2
Sequence CEHXRWGCPPKD

(Modifications: Cys-1 = N-terminal Ac, X = 2-Nal, Asp-12 = C-terminal amide, Disulfide bridge between 1 - 8)

Storage Desiccate at -20°C
CAS Number 207678-81-7
PubChem ID 24821295
InChI Key BRGDPINZISNYJL-VMAVSDBDSA-N
Smiles CC(=O)N[C@H]1CSSC[C@H](NC(=O)CNC(=O)[C@H](CC2=CNC3=C2C=CC=C3)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](CC2=CC3=CC=CC=C3C=C2)NC(=O)[C@H](CC2=CNC=N2)NC(=O)[C@H](CCC(O)=O)NC1=O)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(O)=O)C(N)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solubility Soluble to 1 mg/ml in water

Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Bellasio et al (2003) Melanocortin receptor agonists and antagonists modulate nociceptive sensitivity in the mouse formalin test. Eur.J.Pharmacol. 482 127 PMID: 14660013

Schioth et al (1998) Discovery of novel melanocortin4 receptor selective MSH analogues. Br.J.Pharmacol. 124 75 PMID: 9630346

Whitaker and Reye (2008) Central blockade of melanocortin receptors attenuates the metabolic and locomotor responses to peripheral interleukin-1β administration. Neuropharmacology 54 509 PMID: 18082228


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View Related Products by Product Action

View all Melanocortin (MC) Receptor Antagonists

Keywords: HS 014, HS 014 supplier, Selective, MC4R, receptor, antagonists, Receptors, Melanocortin, HS014, 1831, Tocris Bioscience

1 Citation for HS 014

Citations are publications that use Tocris products. Selected citations for HS 014 include:

Panaro et al (2014) The melanocortin-4 receptor is expressed in enteroendocrine L cells and regulates the release of peptide YY and glucagon-like peptide 1 in vivo. PLoS One 20 1018 PMID: 25453189


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Literature in this Area

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