BMS-470539 dihydrochloride
Based on 1 Customer Validation
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.
- Purity: 99.85%
- CAS No.: 2341796-82-3
- Formula: C32H43Cl2N5O4
- Molecular Weight:632.62
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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MC1R |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wild-type (WT) and MC1 receptor recessive e/e mice induced with ischaemia-reperfusion[3]
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Dosage:2.05 mg/kg, 6.16 mg/kg and 18.47 mg/kg
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Administration:Intravenous injection; for 125 minutes
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Result:Inhibited cell adhesion and emigration with no effect on cell rolling. Inhibited tissue expression of both CXCL1 and CCL2.
Chemical Information
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CAS No. 2341796-82-3
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Appearance Solid
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Molecular Weight 632.62
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Formula C32H43Cl2N5O4
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Color White to off-white
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SMILES
CCCC(C1(C2=CC=CC=C2)CCN(C([C@@H](CC3=CC=C(C=C3)OC)NC([C@H](CC4=CN=CN4C)N)=O)=O)CC1)=O.Cl.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : ≥ 125 mg/mL (197.59 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 100 mg/mL (158.07 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.5807 mL | 7.9036 mL | 15.8073 mL | 39.5182 mL |
| 5 mM | 0.3161 mL | 1.5807 mL | 3.1615 mL | 7.9036 mL | |
| 10 mM | 0.1581 mL | 0.7904 mL | 1.5807 mL | 3.9518 mL | |
| 15 mM | 0.1054 mL | 0.5269 mL | 1.0538 mL | 2.6345 mL | |
| 20 mM | 0.0790 mL | 0.3952 mL | 0.7904 mL | 1.9759 mL | |
| 25 mM | 0.0632 mL | 0.3161 mL | 0.6323 mL | 1.5807 mL | |
| 30 mM | 0.0527 mL | 0.2635 mL | 0.5269 mL | 1.3173 mL | |
| 40 mM | 0.0395 mL | 0.1976 mL | 0.3952 mL | 0.9880 mL | |
| 50 mM | 0.0316 mL | 0.1581 mL | 0.3161 mL | 0.7904 mL | |
| 60 mM | 0.0263 mL | 0.1317 mL | 0.2635 mL | 0.6586 mL | |
| 80 mM | 0.0198 mL | 0.0988 mL | 0.1976 mL | 0.4940 mL | |
| 100 mM | 0.0158 mL | 0.0790 mL | 0.1581 mL | 0.3952 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
BMS-470539 dihydrochloride Related Classifications
HY-115644 Related Classifications
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