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CXCR2-IN-2

Catalog No. T36923 CAS 1838123-21-9

Synonyms: CXCR2-IN-2

CXCR2-IN-2 is a selective CXCR2 antagonist that is brain penetrant and orally bioavailable, with IC50 values of 5.2 nM and 1 nM in the β-arrestin assay and CXCR2 Tango assay, respectively. It exhibits approximately 730-fold selectivity over CXCR1 and greater than 1900-fold selectivity over all other chemokine receptors. Furthermore, CXCR2-IN-2 effectively inhibits Gro-α induced CD11b expression in human whole blood, displaying an IC50 of 0.04 μM[1].

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CXCR2-IN-2, CAS 1838123-21-9

Pack Size	Availability	Price/USD
25 mg	8-10 weeks	$ 1,400.00
50 mg	8-10 weeks	$ 1,820.00
100 mg	8-10 weeks	$ 2,820.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	CXCR2-IN-2 is a selective CXCR2 antagonist that is brain penetrant and orally bioavailable, with IC50 values of 5.2 nM and 1 nM in the β-arrestin assay and CXCR2 Tango assay, respectively. It exhibits approximately 730-fold selectivity over CXCR1 and greater than 1900-fold selectivity over all other chemokine receptors. Furthermore, CXCR2-IN-2 effectively inhibits Gro-α induced CD11b expression in human whole blood, displaying an IC50 of 0.04 μM[1].
Targets&IC50	CXCR1:3.8 μM (IC50), CXCR2:5.2 nM (IC50)
In vivo	CXCR2-IN-2 (compound 68) (1-10 mg/kg; p.o.; twice daily for 3 days) dose-dependently reduces neutrophil infiltration in vivo in rat and mouse air pouch models[1].

Synonyms	CXCR2-IN-2
Molecular Weight	414.9
Formula	C18H23ClN2O5S
CAS No.	1838123-21-9

Storage

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

Solubility Information

DMSO: 240 mg/mL (578.45 mM), Sonication is recommended.

References and Literature

1. Lu H, et al. Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists. J Med Chem. 2018;61(6):2518-2532.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CXCR2-IN-2 1838123-21-9 CXCR2IN2 CXCR2 IN 2 CXCR-2-IN-2 inhibitor inhibit

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