BMS-470539 dihydrochloride

Name: BMS-470539 dihydrochloride
Brand: MedChemExpress
SKU: HY-115644
Rating: 4.5 (1 reviews)

Cat. No.: HY-115644 Purity: 99.95%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 2341796-82-3

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 900	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1450	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

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

In Vitro:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5807 mL	7.9036 mL	15.8073 mL
5 mM	0.3161 mL	1.5807 mL	3.1615 mL
10 mM	0.1581 mL	0.7904 mL	1.5807 mL

View the 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.

* 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.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (279 KB) SDS (252 KB)

COA (257 KB) HNMR (281 KB) LCMS (260 KB)

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

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.