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CCR2 antagonist 5

Catalog No. T27682 CAS 1228650-83-6

Synonyms: JNJ-41443532, JNJ-41443532 Free Base, JNJ 41443532, JNJ41443532

CCR2 antagonist 5 (JNJ-41443532) is a selective and orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM).JNJ-41443532 binds mCCR2 with a Ki of 9.6 µM, which can be used to study inflammatory diseases and diabetes. diseases and diabetes.

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CCR2 antagonist 5, CAS 1228650-83-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 110.00
5 mg	In stock	$ 270.00
10 mg	In stock	$ 400.00
25 mg	In stock	$ 668.00
50 mg	In stock	$ 949.00
100 mg	In stock	$ 1,290.00
500 mg	In stock	$ 2,580.00

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Purity: 98.79%

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Description	CCR2 antagonist 5 (JNJ-41443532) is a selective and orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM).JNJ-41443532 binds mCCR2 with a Ki of 9.6 µM, which can be used to study inflammatory diseases and diabetes. diseases and diabetes.
Targets&IC50	CCR2 (mouse):9.6 μM (Ki), CCR2 (human):37 nM (IC50)
In vivo	CCR2 antagonist 5 (compound 8d) has good CV safety profile. It does not induce dose-dependent or notable effects on most cardiohemodynamic, functional respiratory, and electrophysiological parameters up to 10 mg/kg (i.v.) with plasma level at 70 µM in an anesthetized dog.[1] CCR2 antagonist 5 dose-dependently inhibits the influx of leukocytes, monocytes/macrophages, and T-lymphocytes into the peritoneal cavity with an ED50 of 3 mg/kg p.o. bid in a thioglycollate-induced peritonitis (TG) model.[1] CCR2 antagonist 5 has amendable oral bioavailability in dogs and primates.[1]

Synonyms	JNJ-41443532, JNJ-41443532 Free Base, JNJ 41443532, JNJ41443532
Molecular Weight	482.52
Formula	C22H25F3N4O3S
CAS No.	1228650-83-6

Storage

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

References and Literature

1. Di Prospero NA, Artis E, Andrade-Gordon P, Johnson DL, Vaccaro N, Xi L, Rothenberg P. CCR2 antagonism in patients with type 2 diabetes mellitus: a randomized, placebo-controlled study. Diabetes Obes Metab. 2014 Nov;16(11):1055-64. doi: 10.1111/dom.12309. Epub 2014 May 25. PubMed PMID: 24798870.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Membrane Protein-targeted Compound Library Bioactive Compounds Library Max Bioactive Compound Library Immunology/Inflammation Compound Library

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Related compounds with same targets

CCR1 antagonist 8 J-113863 Cenicriviroc Mesylate MK-0812 ML604086 SB 328437 Cenicriviroc JAK-IN-3

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Keywords

CCR2 antagonist 5 1228650-83-6 Immunology/Inflammation Microbiology/Virology CCR JNJ-41443532 JNJ-41443532 Free Base JNJ 41443532 JNJ41443532 inhibitor inhibit

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