BMS-470539 dihydrochloride

Name: BMS-470539 dihydrochloride
Brand: MedChemExpress
SKU: HY-115644
Rating: 4.5 (0 reviews)

Cat. No.: HY-115644 Purity: 99.85%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

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BMS-470539 dihydrochloride 화학구조

CAS No. : 2341796-82-3

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

or 대량구매 문의

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 1 Customer Validation

Other Forms of BMS-470539 dihydrochloride:

BMS-470539 견적 받기

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Melanocortin Receptor Isoform Specific Products:

View All Isoforms

MC1R MC3R MC2R MC4R MC5R

Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target

MC1R

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.

분자량

632.62

화학식

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

선적

Room temperature in continental US; may vary elsewhere.

보관

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

용액&용해도

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.

몰농도 계산기
농도 희석 계산기

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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).

순도&문서

Purity: 99.85%

Select Batch:

Data Sheet (279 KB) SDS (252 KB)

COA (257 KB) HNMR (324 KB) LCMS (92 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.