Art. -Nr.: HY-112792

CCR2 antagonist 1

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CCR2 antagonist 1 (compound 15a) is a high-affinity and long-residence-time CCR2 antagonist, with a K_i of 2.4 nM.

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Reinheit: 95.04%
CAS. Nr.: 1683534-96-4
Formel: C₂₈H₃₂BrF₃N₂O
Molecular Weight:549.47

Speicherung:

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

CCR2 antagonist 1 Chemical Structure

CAS. Nr.: 1683534-96-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

CCR2 antagonist 1 (compound 15a) is a high-affinity and long-residence-time CCR2 antagonist, with a K_i of 2.4 nM^[1].

IC₅₀ & Target^[1]

CCR2

2.4 nM (Ki)

Alle CCR Isoform-spezifische Produkte anzeigen :

In Vitro

The combination of SAR and SKR in the hit-to-lead process results in the discovery of a new higheaffinity and longeresidenceetime CCR2 antagonist (CCR2 antagonist 1 (compound 15a), K_i=2.4 nM; RT=714 min)^[1].

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

Chemical Information

CAS. Nr. 1683534-96-4
Appearance Solid
Molecular Weight 549.47
Formel C₂₈H₃₂BrF₃N₂O
Color Light yellow to yellow
SMILES

O=C([C@]1(C(C)C)C[C@H](N[C@@H]2CCC3=C2C=CC(Br)=C3)CC1)N4CC5=C(C=CC(C(F)(F)F)=C5)CC4
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (1)

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Sci Adv

CCR2 is a host entry receptor for severe fever with thrombocytopenia syndrome virus. [Abstract]

2023 Aug 2;9(31):eadg6856. PMID: 37531422

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (227.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8199 mL

9.0997 mL

18.1994 mL

5 mM

0.3640 mL

1.8199 mL

3.6399 mL

10 mM

0.1820 mL

0.9100 mL

1.8199 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: 5% DMSO 45% PEG300 50% Water

Solubility: 11 mg/mL (20.02 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Vilums M, et al. When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as CCR2 antagonists. Eur J Med Chem. 2015 Mar 26;93:121-34. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8199 mL	9.0997 mL	18.1994 mL	45.4984 mL
	5 mM	0.3640 mL	1.8199 mL	3.6399 mL	9.0997 mL
	10 mM	0.1820 mL	0.9100 mL	1.8199 mL	4.5498 mL
	15 mM	0.1213 mL	0.6066 mL	1.2133 mL	3.0332 mL
	20 mM	0.0910 mL	0.4550 mL	0.9100 mL	2.2749 mL
	25 mM	0.0728 mL	0.3640 mL	0.7280 mL	1.8199 mL
	30 mM	0.0607 mL	0.3033 mL	0.6066 mL	1.5166 mL
	40 mM	0.0455 mL	0.2275 mL	0.4550 mL	1.1375 mL
	50 mM	0.0364 mL	0.1820 mL	0.3640 mL	0.9100 mL
	60 mM	0.0303 mL	0.1517 mL	0.3033 mL	0.7583 mL
	80 mM	0.0227 mL	0.1137 mL	0.2275 mL	0.5687 mL
	100 mM	0.0182 mL	0.0910 mL	0.1820 mL	0.4550 mL

Keywords

CCR2 antagonist 1

1 Cited Publications

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CCR2 antagonist 1

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Publications Citing Use of MedChemExpress (MCE) CCR2 antagonist 1

Alle CCR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CCR2 antagonist 1

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Small Molecule Immuno-Oncology Compound Library

Endocrinology Compound Library

Targeted Diversity Library

Anti-Pulmonary Fibrosis Compound Library

Chemokine Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) CCR2 antagonist 1

Alle CCR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CCR2 antagonist 1 Related Classifications

HY-112792 Related Classifications