Chemistry:BMS-470539
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Short description: Chemical compound
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| Routes of administration | S.C.[1] |
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| Bioavailability | 100% (with S.C. administration)[1] |
| Elimination half-life | 1.7 hours[1] |
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| Formula | C32H41N5O4 |
| Molar mass | 559.711 g·mol−1 |
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BMS-470539 is a small-molecule experimental drug which acts as a potent and highly selective full agonist of the MC1 receptor.[1][2] It was discovered in 2003 as part of an effort to understand the role of the MC1 receptor in immunomodulation, and has since been used in scientific research to determine its role in inflammatory processes.[1][2][3] The compound was designed with the intention of mimicking the central His-Phe-Arg-Trp pharmacophore of the melanocortins,[1][2] and this proved to be successful based on its favorable pharmacodynamic profile.
See also
References
- ↑ 1.0 1.1 1.2 1.3 1.4 1.5 "A selective small molecule agonist of the melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice". Journal of Leukocyte Biology 80 (4): 897–904. October 2006. doi:10.1189/jlb.1204748. PMID 16888084. http://www.jleukbio.org/cgi/pmidlookup?view=long&pmid=16888084.
- ↑ 2.0 2.1 2.2 "Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties". Journal of Medicinal Chemistry 46 (7): 1123–6. March 2003. doi:10.1021/jm025600i. PMID 12646021.
- ↑ "The melanocortin MC(1) receptor agonist BMS-470539 inhibits leucocyte trafficking in the inflamed vasculature". British Journal of Pharmacology 160 (1): 171–80. May 2010. doi:10.1111/j.1476-5381.2010.00688.x. PMID 20331604.
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