Reagenzien und Instrumente für die Immunologie Zellbiologie und Molekularbiologie

RS 504393 [300816-15-3]

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Katalog-Nummer HY-15418-5mg

Size : 5mg

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Marke : MedChemExpress

Contact local distributor :

Telefonnummer : +1 850 650 7790

RS 504393 is a selective CCR2 chemokine receptor antagonist (IC₅₀ values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively).

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RS 504393 Chemische Struktur

CAS. Nr. : 300816-15-3

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

Based on 18 publication(s) in Google Scholar

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Beschreibung

RS 504393 is a selective CCR2 chemokine receptor antagonist (IC₅₀ values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively).

IC₅₀ & Target^[5]

CCR2

89 nM (IC₅₀)

Human α_1a receptor

72 nM (IC₅₀)

Human α_1d receptor

460 nM (IC₅₀)

5HT-1a receptor

1070 nM (IC₅₀)

In Vitro

RS 504393 inhibits the MCP-1-induced chemotaxis with an IC₅₀ of 330 nM. RS 504393 treatment suppresses allergen induced β-hexosaminidase release significantly. Without allergen priming, MCP-1 induces mast cell degranulation, which is completely suppressed by RS 504393^[4].

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

In Vivo

RS504393 (0.3-3 μg) with CCL2 progressively blocks thermal hyperalgesia dose-dependently in mice^[1]. RS 504393 (5 mg/kg, i.v.) supresses the elevated numbers of leukocytes and increased total protein content in BALF induced by The LPS. RS504393 significantly down regulates the LPS-induced elevation of IL-1β, PAI-1 mRNA and protein expressions. RS504393 significantly suppresses induced lung edema, protein-rich fluid, polymorphonuclear accumulation and bronchial wall thickening induced by LPS^[2]. RS-504393 significantly reduces renal pathology, especially the extensive interstitial fibrosis mediated by decrease in type I collagen synthesis in a UUO model^[3].

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

Molekulargewicht

417.50

Formel

C₂₅H₂₇N₃O₃

CAS. Nr.

300816-15-3

Appearance

Solid

Color

White to off-white

SMILES

O=C1NC2=CC=C(C)C=C2C3(CCN(CCC4=C(C)OC(C5=CC=CC=C5)=N4)CC3)O1

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 10 mg/mL (23.95 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 1 mg/mL (2.40 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3952 mL	11.9760 mL	23.9521 mL
5 mM	0.4790 mL	2.3952 mL	4.7904 mL
10 mM	0.2395 mL	1.1976 mL	2.3952 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* 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.

Molaritätsrechner
Verdünnungsrechner

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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% DMSO 15% EtOH 35% PEG300
Solubility: 31.25 mg/mL (74.85 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (2.99 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (2.99 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Reinheit & Dokumentation

Purity: 99.43%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (252 KB) HNMR (262 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

Verweise

[1]. Baamonde, Ana., et al. Involvement of glutamate NMDA and AMPA receptors, glial cells and IL-1β in the spinal hyperalgesia evoked by the chemokine CCL2 in mice. Neuroscience Letters (2011), 502(3), 178-181. [Content Brief]

[2]. Yang, Dong., et al. Roles of CC chemokine receptors (CCRs) on lipopolysaccharide-induced acute lung injury. Respiratory Physiology & Neurobiology (2010), 170(3), 253-259. [Content Brief]

[3]. Kitagawa, Kiyoki., et al. Blockade of CCR2 ameliorates progressive fibrosis in kidney. American Journal of Pathology (2004), 165(1), 237-246. [Content Brief]

[4]. Tominaga T, et al. Blocking mast cell-mediated type I hypersensitivity in experimental allergic conjunctivitis by monocyte chemoattractant protein-1/CCR2. Invest Ophthalmol Vis Sci. 2009 Nov;50(11):5181-8. [Content Brief]

[5]. Mirzadegan T, et al. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle. J Biol Chem. 2000 Aug 18;275(33):25562-71. [Content Brief]

Kinase-Assay ^[4]	Isolated mast cells are sensitized by incubation with anti-DNP IgE in RPMI1640 containing 10 ng/mL of murine recombinant IL-3, 10 ng/mL of recombinant SCF, and 5% murine serum. The cells are then washed with HBSS containing 10 ng/mL of murine recombinant IL-3, 10 ng/mL of recombinant SCF, 0.04% BSA, and 10 mM HEPES. Resuspended cells at a concentration of 2 to 8×10⁴ cells/100 μL are transferred into triplicate wells of a 96 well U-bottom plate and allowed to equilibrate at 37°C for 10 minutes before the addition of DNP-albumin or compound 48/80. After 45 minutes, the plate is centrifuged at 290 g for 5 minutes at 4°C. The β-hexosaminidase activity of the culture supernatant is determined using a Published protocol. Fifty-μL aliquots of the supernatant are placed in wells of another 96-well plate together with 100 μL of 2.5 mM p-nitrophenyl-N-acetyl β-d glucosaminide solubilized in 0.04mol/Lcitrate buffer adjusted to pH 4.5 with disodium phosphate. After incubation at 37°C for 90 minutes, the reactions are terminated by addition of 50 μL of 0.4mol/Lglycin adjusted to pH 10.7 with sodium hydroxide. The colored product is measured at 405 nm with a reference filter of 570 nm. The relative release of β-hexosaminidase is defined as the activity in the supernatant of the tested cells divided by the activity in the positive control cell supernatant, multiplied by 100. Compound 48/80 stimulus is used for assay control. MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.
Tierverwaltung ^[2]	Male C57BL/6J mice (n=30) and male homozygote CCR1, CCR2 and CCR3 knockout mice (n=12, in each phenotype), 6-8 weeks old and weighing 20±2 g. Intranasal administration of PBS or LPS (5 mg/kg) is performed in a volume of 1 mL/kg body weight. C57BL/6J mice are treated with vehicle or RS504393 (5 mg/kg) intraperitoneally 30 min before LPS challenge. Four hours after LPS challenge, mice are terminated by an intraperitoneal injection of an overdose of pentobarbitone. The mice are kept on a 12-h light/dark cycle with access to mice chow and water ad libitum. MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.
Verweise	[1]. Baamonde, Ana., et al. Involvement of glutamate NMDA and AMPA receptors, glial cells and IL-1β in the spinal hyperalgesia evoked by the chemokine CCL2 in mice. Neuroscience Letters (2011), 502(3), 178-181. [Content Brief] [2]. Yang, Dong., et al. Roles of CC chemokine receptors (CCRs) on lipopolysaccharide-induced acute lung injury. Respiratory Physiology & Neurobiology (2010), 170(3), 253-259. [Content Brief] [3]. Kitagawa, Kiyoki., et al. Blockade of CCR2 ameliorates progressive fibrosis in kidney. American Journal of Pathology (2004), 165(1), 237-246. [Content Brief] [4]. Tominaga T, et al. Blocking mast cell-mediated type I hypersensitivity in experimental allergic conjunctivitis by monocyte chemoattractant protein-1/CCR2. Invest Ophthalmol Vis Sci. 2009 Nov;50(11):5181-8. [Content Brief] [5]. Mirzadegan T, et al. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle. J Biol Chem. 2000 Aug 18;275(33):25562-71. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.3952 mL	11.9760 mL	23.9521 mL	59.8802 mL
DMSO	5 mM	0.4790 mL	2.3952 mL	4.7904 mL	11.9760 mL
	10 mM	0.2395 mL	1.1976 mL	2.3952 mL	5.9880 mL
	15 mM	0.1597 mL	0.7984 mL	1.5968 mL	3.9920 mL
	20 mM	0.1198 mL	0.5988 mL	1.1976 mL	2.9940 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.

RS 504393 [300816-15-3]

Katalog-Nummer HY-15418-5mg

Contact local distributor :

Marke : MedChemExpress

Contact local distributor :

Alle CCR Isoform-spezifische Produkte anzeigen:

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

RS 504393 Related Classifications

Keywords:

Sie könnten auch an folgenden Produkten interessiert sein:

RS 504393 [300816-15-3]

Katalog-Nummer HY-15418-5mg

Contact local distributor :

Marke : MedChemExpress

Contact local distributor :

Alle CCR Isoform-spezifische Produkte anzeigen:

RS 504393 Related Antibodies

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

RS 504393 Related Classifications

Keywords:

Sie könnten auch an folgenden Produkten interessiert sein: