| Identification | Back Directory | [Name]
BMS-470539 dihydrochloride | [CAS]
2341796-82-3 | [Synonyms]
BMS470539 dihydrochloride,BMS 470539 dihydrochloride
BMS-470539 dihydrochloride, BMS 470539 dihydrochloride, BMS470539 dihydrochloride, BMS 470539 HCl | [Molecular Formula]
C32H42ClN5O4 | [MOL File]
2341796-82-3.mol | [Molecular Weight]
596.17 |
| Chemical Properties | Back Directory | [storage temp. ]
-10 to -25°C | [solubility ]
DMSO:63.26(Max Conc. mg/mL);100.0(Max Conc. mM)
Water:63.26(Max Conc. mg/mL);100.0(Max Conc. mM) | [form ]
A crystalline solid | [color ]
White to off-white | [Water Solubility ]
H2O: 2mg/mL, clear (Warmed) | [SMILES]
CCCC(C1(C2=CC=CC=C2)CCN(CC1)C([C@H](NC([C@@H](N)CC3=CN=CN3C)=O)CC4=CC=C(C=C4)OC)=O)=O.[2HCl] |
| Hazard Information | Back Directory | [Uses]
BMS-470539 dihydrochloride is a highly potent and selective melanocortin-1 receptor (MC-1R) agonist with an IC50 of 120 nM, an EC50 of 28 nM. BMS-470539 dihydrochloride does not activate MC-3R and is a very weak partial agonist at MC-4R and MC-5R. BMS-470539 dihydrochloride has potently anti-inflammatory properties[1][2][3]. | [Biological Activity]
BMS-470539 is a highly potent and selective melanocortin-1 receptor (MC-1R; MC1R) agonist (AMP stimulation EC50 = 11.6/16.2/16.8 nM using B16/HBL/CHO-MC1R; little or no potency toward MC2RMC3R MC4R MC5R) with anti-inflammatory efficacy in mice in vivo (15-100 μmol/kg via i.v. or s.c. 0.5-1 h prior to 1 μg LPS s.c.). | [in vivo]
BMS-470539 (2.05-18.47 mg/kg; intravenous injection; for 125 minutes; WT and MC1 receptor recessive e/e mice) treatment inhibits cell adhesion and emigration with no effect on cell rolling. And also inhibits the tissue expression of both CXCL1 and CCL2[3]. | Animal Model: | Wild-type (WT) and MC1 receptor recessive e/e mice induced with ischaemia-reperfusion[3] | | Dosage: | 2.05 mg/kg, 6.16 mg/kg and 18.47 mg/kg | | Administration: | Intravenous injection; for 125 minutes | | Result: | Inhibited cell adhesion and emigration with no effect on cell rolling. Inhibited tissue expression of both CXCL1 and CCL2.
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| [IC 50]
MC1R | [References]
[1] Herpin TF, et al. Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties. J Med Chem. 2003 Mar 27;46(7):1123-6. DOI:10.1021/jm025600i
[2] Kang L, et al. A selective small molecule agonist of the melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice. J Leukoc Biol. 2006 Oct;80(4):897-904. Epub 2006 Aug 3. DOI:10.1189/jlb.1204748
[3] Leoni G, et al. The melanocortin MC(1) receptor agonist BMS-470539 inhibits leucocyte trafficking in the inflamed vasculature. Br J Pharmacol. 2010 May;160(1):171-80. DOI:10.1111/j.1476-5381.2010.00688.x |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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