BMS-470539 (dihydrochloride)

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

製品番号: HY-115644 純度: 99.85%: Data Sheet SDS COA 取扱説明書
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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

BMS-470539 (dihydrochloride) 構造式

CAS 番号 : 2341796-82-3

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 209	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 209	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$150	在庫あり	Estimated Time of Arrival: December 31
10 mg	$250	在庫あり	Estimated Time of Arrival: December 31
25 mg	$550	在庫あり	Estimated Time of Arrival: December 31
50 mg	$900	在庫あり	Estimated Time of Arrival: December 31
100 mg	$1450	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

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

カスタマーレビュー

Based on 0 publication(s) in Google Scholar

Other Forms of BMS-470539 dihydrochloride:

BMS-470539 お問い合わせ

Melanocortin Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

MC1R MC3R MC2R MC4R MC5R

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

MC1R

体外実験

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.

体内実験

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.

分子量

632.62

分子式

C₃₂H₄₃Cl₂N₅O₄

CAS 番号

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

-20°C, sealed storage, away from moisture

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

溶剤 & 溶解度

体外:

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.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

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).

純度とドキュメンテーション

純度: 99.85%

Select Batch:

データシート (279 KB) SDS (252 KB)

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

取扱説明書 (2659 KB)

参考文献

[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.