1. GPCR/G Protein
    Neuronal Signaling
  2. Melanocortin Receptor
  3. BMS-470539 dihydrochloride

BMS-470539 dihydrochloride 

Cat. No.: HY-115644 Purity: 98.50%
Handling Instructions

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.

For research use only. We do not sell to patients.

BMS-470539 dihydrochloride Chemical Structure

BMS-470539 dihydrochloride Chemical Structure

CAS No. : 2341796-82-3

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Description

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].

IC50 & Target

IC50: 120 nM (Melanocortin-1 receptor); EC50: 28 nM (Melanocortin-1 receptor)[1]

In Vitro

An HBL melanoma cell line is established that stably expresses a NF-κB luciferase reporter. In these cells, 0.5 ng/mL TNF-α induces a dose-dependent increase in NF-κB luciferase activity. Treatment of HBL-NF-κB cells with BMS-470539 elicits a dose-dependent, statistically significant reduction in TNF-α-stimulated NF-κB luciferase activity. BMS-470539 has no effect on luciferase reporter activity in the absence of TNF-α stimulation. In nontransfected HBL cells, treatment with BMS-470539 results in a dose-dependent inhibition of NF-B nuclear translocation[2].

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.
Molecular Weight

632.62

Formula

C₃₂H₄₃Cl₂N₅O₄

CAS No.

2341796-82-3

SMILES

CCCC(C1(C2=CC=CC=C2)CCN(C([[email protected]@H](CC3=CC=C(C=C3)OC)NC([[email protected]](CC4=CN=CN4C)N)=O)=O)CC1)=O.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: 98.50%

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Keywords:

BMS-470539BMS470539BMS 470539Melanocortin ReceptorMC ReceptorMC-1Ranti-inflammatoryadhesionemigration,CXCL1CCL2ischaemia-reperfusionNF-κBTNF-αInhibitorinhibitorinhibit

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BMS-470539 dihydrochloride
Cat. No.:
HY-115644
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