BMS CCR2 22

Modify Date: 2024-02-02 13:03:10

BMS CCR2 22 Structure
BMS CCR2 22 structure
Common Name BMS CCR2 22
CAS Number 445479-97-0 Molecular Weight 593.66100
Density N/A Boiling Point N/A
Molecular Formula C28H34F3N5O4S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of BMS CCR2 22


BMS CCR2 22 is a potent, specific and high affinity CC-type chemokine receptor 2 (CCR2) antagonist with excellent binding affinity (binding IC50 of 5.1 nM) and potent functional antagonism (calcium flux IC50 of 18 nM and chemotaxis IC50 of 1 nM)[1][2].

 Names

Name N-[2-[[(1R,2S)-2-[(4-methylsulfanylbenzoyl)amino]cyclohexyl]amino]-2-oxoethyl]-2-(propan-2-ylcarbamoylamino)-5-(trifluoromethyl)benzamide
Synonym More Synonyms

 BMS CCR2 22 Biological Activity

Description BMS CCR2 22 is a potent, specific and high affinity CC-type chemokine receptor 2 (CCR2) antagonist with excellent binding affinity (binding IC50 of 5.1 nM) and potent functional antagonism (calcium flux IC50 of 18 nM and chemotaxis IC50 of 1 nM)[1][2].
Related Catalog
Target

CCR2:5.1 nM (IC50)

In Vitro BMS CCR2 22 (Compound 22) has binding affinity for wild-type and E291A mutants with IC50 values of 7.5 nM and 3.7 nM, respectively[1].BMS CCR2 22 prevents both the binding and the internalization of fluorescently labeled hMCP-1_AF647 internalization in human monocytes. BMS CCR2 22 inhibits the internalization of hMCP1_AF647 with an IC50 value of approximately 2 nM[2]. The addition of BMS CCR2 22 (0.1-10 μM; 24 h), cenicriviroc (CVC) or a combination of both BMS CCR2 22 and MVC to human aortic endothelial cells (HAoECs) prior to MCP-1 stimulation do not alter E-selectin, ICAM-1, or CD99 cell surface expression. Incubation of HAoECs with BMS CCR2 22 before MCP-1 significantly increases VCAM-1 and PECAM1 cell surface levels (from 72.8 to 160% and from 97.2 and 127%, respectively)[3].
References

[1]. Cherney RJ, et al. Discovery of disubstituted cyclohexanes as a new class of CC chemokine receptor 2 antagonists. J Med Chem. 2008 Feb 28;51(4):721-4.

[2]. Kredel S, et al. High-content analysis of CCR2 antagonists on human primary monocytes. J Biomol Screen. 2011 Aug;16(7):683-93.

[3]. D'Antoni ML, et al. Cenicriviroc inhibits trans-endothelial passage of monocytes and is associated with impaired E-selectin expression. J Leukoc Biol. 2018 Dec;104(6):1241-1252.

 Chemical & Physical Properties

Molecular Formula C28H34F3N5O4S
Molecular Weight 593.66100
Exact Mass 593.22800
PSA 153.73000
LogP 6.18100

 Synonyms

Carboxy-PTIO,potassium salt
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  • DC Chemicals Limited
  • China
  • Product Name: BMS-22
  • Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
  • Purity: 98.0%
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  • Contact: Tony Cao

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Price: ¥2100/1 mg

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