BMS 470539 (hydrochloride) |
| Catalog No.GC42954 |
BMS 470539 is an agonist of melanocortin receptor 1 (MC1R) with EC50 values of 16.8 and 11.6 nM for human and murine MC1R, respectively, in a cAMP accumulation assay.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2341796-82-3
Sample solution is provided at 25 µL, 10mM.
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BMS 470539 is an agonist of melanocortin receptor 1 (MC1R) with EC50 values of 16.8 and 11.6 nM for human and murine MC1R, respectively, in a cAMP accumulation assay. [1] It inhibits TNF-α-induced NF-κB activation in vitro in a dose-dependent manner. In vivo, subcutaneous administration of BMS 470539 inhibits LPS-induced TNF-α production in wild-type mice (ED50 = 10 μmol/kg). It reduces LPS-induced leukocyte infiltration and paw swelling in mouse models of lung inflammation and delayed-type hypersensitivity, respectively. BMS 470539 administration also decreases retinal damage in a mouse model of streptozotocin-induced diabetic retinopathy. [2]
Reference:
[1]. Kang, L., McIntyre, K.W., Gillooly, K.M., 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. 80(4), 897-904 (2006).
[2]. Rossi, S., Maisto, R., Gesualdo, C., et al. Activation of melanocortin receptors MC1 and MC5 attenuates retinal damage in experimental diabetic retinopathy. Mediators Inflamm.
| Cas No. | 2341796-82-3 | SDF | |
| Chemical Name | 1-[1-(3-methyl-L-histidyl-O-methyl-D-tyrosyl)-4-phenyl-4-piperidinyl]-1-butanone, dihydrochloride | ||
| Canonical SMILES | O=C([C@@H](CC1=CC=C(OC)C=C1)NC([C@@H](N)CC2=CN=CN2C)=O)N3CCC(C4=CC=CC=C4)(C(CCC)=O)CC3.Cl.Cl | ||
| Formula | C32H41N5O4•2HCl | M.Wt | 632.6 |
| Solubility | DMF: 25 mg/ml, DMSO: 10 mg/ml, Ethanol: 20 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5808 mL | 7.9039 mL | 15.8078 mL |
| 5 mM | 0.3162 mL | 1.5808 mL | 3.1616 mL |
| 10 mM | 0.1581 mL | 0.7904 mL | 1.5808 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)
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