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CCR2-RA-[R]

Catalog No. T14900 CAS 512177-83-2

CCR2-RA-[R] is a C-C chemokine receptor type 2 (CCR2) allosteric antagonist (IC50: 103 nM).

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CCR2-RA-[R], CAS 512177-83-2

Pack Size	Availability	Price/USD
2 mg	In stock	$ 39.00
5 mg	In stock	$ 64.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 197.00
50 mg	In stock	$ 320.00
100 mg	In stock	$ 441.00
1 mL * 10 mM (in DMSO)	In stock	$ 70.00

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Purity: 99.65%

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Description	CCR2-RA-[R] is a C-C chemokine receptor type 2 (CCR2) allosteric antagonist (IC50: 103 nM).
Targets&IC50	CCR2:103 nM (in U2OS-CCR2 cells)
In vitro	CCR2-RA-[R] inhibits CCR2 non-competitively by blocking activation-associated conformational changes and formation of the G protein-binding interface. CCR2-RA-[R] displaces [125I]CCL2 from CCR2 with an pIC50 value of 6.1. The pKD of CCR2-RA-[R] for CCR2 and CCR5 is 8.8±0.1 and 7.0±0.1, respectively[2]. The chemokine receptor CCR2 is a G protein-coupled receptor that is involved in many diseases characterized by chronic inflammation, and therefore a large variety of CCR2 small molecule antagonists has been developed. The binding pocket of CCR2-RA-[R] is highly enclosed and possesses a balanced combination of hydrophobic and polar features, all of which favors pocket “druggability”[3].

Molecular Weight	351.8
Formula	C18H19ClFNO3
CAS No.	512177-83-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 0.1 mg/mL (insoluble)

DMSO: 125 mg/mL (355.32 mM)

References and Literature

1. Zweemer AJ, et al. Multiple binding sites for small-molecule antagonists at the CC chemokine receptor 2. Mol Pharmacol. 2013 Oct;84(4):551-61. 2. Zweemer AJ, et al. Discovery and mapping of an intracellular antagonist binding site at the chemokine receptor CCR2. Mol Pharmacol. 2014 Oct;86(4):358-68. 3. Zheng Y, et al. Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists. Nature. 2016 Dec 15;540(7633):458-461.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library NO PAINS Compound Library Immuno-Oncology Compound Library Immunology/Inflammation Compound Library Bioactive Compound Library Bioactive Compounds Library Max Covalent Inhibitor Library Cytokine Inhibitor Library Chemokine Inhibitor Library

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CCR1 antagonist 8 BMS-817399 RS102895 hydrochloride MLN-3897 CCR5 antagonist 1 GW 766994 MK-0812 Succinate 5-Hydroxy-7,8-dimethoxyflavanone

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Keywords

CCR2-RA-[R] 512177-83-2 Immunology/Inflammation Microbiology/Virology CCR Inhibitor inhibit CCR-2-RA-[R] CC chemokine receptor CCR2RA[R] CCR2 RA [R] inhibitor

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