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NBI-74330 is a chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist with a Ki value of 3.6 nM in a radioligand binding assay. It effectively inhibits calcium mobilization induced by chemokine (C-X-C motif) ligand 10 (CXCL10) or CXCL11 in RBL cells expressing human CXCR3, with IC50 values of 7 nM for both. Additionally, NBI-74330 inhibits CXCL11-induced chemotaxis of CXCR3-expressing H9 cells and PHA and IL-2 differentiated T cells, with IC50s of 3.9 and 6.6 nM, respectively. In vivo, it has been shown to reduce peritoneal lymphocyte migration in a mouse model of peritonitis, decrease the size and number of aortic arch atherosclerotic lesions in Ldlr-/mice, and reduce spinal cord microglial activation and levels of CXCL4, CXCL9, and CXCL10, as well as decrease thermal and mechanical hyperalgesia in a rat model of chronic constriction injury-induced neuropathic pain.

855527-92-3

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855527-92-3 Usage

Uses

Used in Pharmaceutical Industry:
NBI-74330 is used as a CXCR3 antagonist for the treatment of various inflammatory and immune-related conditions. Its ability to inhibit chemotaxis and reduce inflammation makes it a potential candidate for the development of therapeutic agents targeting diseases such as atherosclerosis, peritonitis, and neuropathic pain.
Used in Research Applications:
NBI-74330 is used as a research tool for studying the role of CXCR3 in various biological processes and disease mechanisms. Its high affinity and selectivity for CXCR3 make it a valuable compound for investigating the molecular and cellular functions of this receptor in both in vitro and in vivo experimental models.

Check Digit Verification of cas no

The CAS Registry Mumber 855527-92-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,5,5,5,2 and 7 respectively; the second part has 2 digits, 9 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 855527-92:
(8*8)+(7*5)+(6*5)+(5*5)+(4*2)+(3*7)+(2*9)+(1*2)=203
203 % 10 = 3
So 855527-92-3 is a valid CAS Registry Number.

855527-92-3SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 18, 2017

Revision Date: Aug 18, 2017

1.Identification

1.1 GHS Product identifier

Product name N-{1-[3-(4-Ethoxyphenyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin- 2-yl]ethyl}-2-[4-fluoro-3-(trifluoromethyl)phenyl]-N-(3-pyridinyl methyl)acetamide

1.2 Other means of identification

Product number -
Other names -

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

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More Details:855527-92-3 SDS

855527-92-3Downstream Products

855527-92-3Relevant academic research and scientific papers

Synthesis and Application of the First Radioligand Targeting the Allosteric Binding Pocket of Chemokine Receptor CXCR3

Bernat, Viachaslau,Heinrich, Markus R.,Baumeister, Paul,Buschauer, Armin,Tschammer, Nuska

, p. 1481 - 1489 (2012/10/08)

Strategies for the identification of allosteric modulators of chemokine receptors largely rely on various cell-based functional assays. Radioligand binding assays are typically not available for allosteric binding sites. We synthesized, purified, and appl

Optimization of a series of quinazolinone-derived antagonists of CXCR3

Liu, Jiwen,Fu, Zice,Li, An-Rong,Johnson, Michael,Zhu, Liusheng,Marcus, Andrew,Danao, Jay,Sullivan, Tim,Tonn, George,Collins, Tassie,Medina, Julio

scheme or table, p. 5114 - 5118 (2010/03/31)

The evaluation of the CXCR3 antagonist AMG 487 in clinic trials was complicated due to the formation of an active metabolite. In this Letter, we will discuss the further optimization of the quinazolinone series that led to the discovery of compounds devoi

Synthesis and structure-activity relationships of 3H-quinazolin-4-ones and 3H-pyrido[2,3-d]pyrimidin-4-ones as CXCR3 receptor antagonists

Storelli, Stefania,Verzijl, Dennis,Al-Badie, Jawad,Elders, Niels,Bosch, Leontien,Timmerman, Henk,Smit, Martine J.,De Esch, Iwan J. P.,Leurs, Rob

, p. 281 - 291 (2008/02/10)

CXC chemokine receptor-3 (CXCR3) is a G-protein coupled receptor (GPCR) predominantly expressed on activated T lymphocytes that promote Th1 responses. Previously, we described the 3H-quinazolin-4-one containing VUF 5834 (decanoic acid {1-[3-(4-cyano-pheny

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