NBI-74330 - CAS 855527-92-3
Catalog number: 855527-92-3
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
A small molecule antagonist for CXCR3
Publictions citing BOC Sciences Products
  • >> More
Brife Description:
A small molecule antagonist for CXCR3
Light yellow to yellow Solid
in DMSO > 10 mM
Please store the product under the recommended conditions in the Certificate of Analysis.
Quality Standard:
Canonical SMILES:
1.Analysis of the pharmacokinetic/pharmacodynamic relationship of a small molecule CXCR3 antagonist, NBI-74330, using a murine CXCR3 internalization assay.
Jopling LA1, Watt GF, Fisher S, Birch H, Coggon S, Christie MI. Br J Pharmacol. 2007 Dec;152(8):1260-71. Epub 2007 Nov 5.
BACKGROUND AND PURPOSE: Pharmacokinetic/pharmacodynamic (PK/PD) models are necessary to relate the degree of drug exposure in vivo to target blockade and pharmacological efficacy. This manuscript describes a murine agonist-induced CXCR3 receptor internalization assay and demonstrates its utility for PK/PD analyses.
2.Identification of overlapping but differential binding sites for the high-affinity CXCR3 antagonists NBI-74330 and VUF11211.
Scholten DJ1, Roumen L, Wijtmans M, Verkade-Vreeker MC, Custers H, Lai M, de Hooge D, Canals M, de Esch IJ, Smit MJ, de Graaf C, Leurs R. Mol Pharmacol. 2014 Jan;85(1):116-26. doi: 10.1124/mol.113.088633. Epub 2013 Oct 30.
CXC chemokine receptor CXCR3 and/or its main three ligands CXCL9, CXCL10, and CXCL11 are highly upregulated in a variety of diseases. As such, considerable efforts have been made to develop small-molecule receptor CXCR3 antagonists, yielding distinct chemical classes of antagonists blocking binding and/or function of CXCR3 chemokines. Although it is suggested that these compounds bind in an allosteric fashion, thus far no evidence has been provided regarding the molecular details of their interaction with CXCR3. Using site-directed mutagenesis complemented with in silico homology modeling, we report the binding modes of two high-affinity CXCR3 antagonists of distinct chemotypes: VUF11211 [(S)-5-chloro-6-(4-(1-(4-chlorobenzyl)piperidin-4-yl)-3-ethylpiperazin-1-yl)-N-ethylnicotinamide] (piperazinyl-piperidine) with a rigid elongated structure containing two basic groups and NBI-74330 [(R)-N-(1-(3-(4-ethoxyphenyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-2-yl)ethyl)-2-(4-fluoro-3-(trifluoromethyl)phenyl)-N-(pyridin-3-ylmethyl)acetamide] (8-azaquinazolinone) without any basic group.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related CXCR Products

(CAS: 568526-77-2)

KRH1636 is an orally active, selective and extremely potent CXC chemokine receptor 4(CXCR4) antagonist. It exhibits a potent and selective anti-HIV-1 activity. ...

CAS 113558-15-9 Baohuoside I

Baohuoside I
(CAS: 113558-15-9)

A regulator of CXCR4 expression

CAS 185991-07-5 AMD3465 hexahydrobromide

AMD3465 hexahydrobromide
(CAS: 185991-07-5)

AMD3465 is a potent and highly selective monomacrocyclic CXCR4 antagonist (IC50= 0.75 nM). It potently inhibits HIV cell entry in vitro and causes leukocytosis ...

CAS 473727-83-2 SCH 527123

SCH 527123
(CAS: 473727-83-2)

A potent antagonist of both CXCR1 and CXCR2 with IC50 of 42 nM and 3 nM, respectively.

AMD 3465
(CAS: 185991-24-6)

AMD 3465,a N-pyridinylmethylene monocyclam, is a selective antagonist of CXCL12/CXCR4-mediated interactions including ligand binding and receptor activation. Wi...

ATI 2341
(CAS: 1337878-62-2)

CXCR4 allosteric agonist

CTCE 9908
(CAS: 1030384-98-5)

CXCR4 antagonist; Induces mitotic catastrophe in ovarian cancer cells

(CAS: 864677-55-4)

IT1t is a selective CXCR4 antagonist with IC50 value of 1.1 nM in calcium mobilization assays.It may be potential useful as anti-HIV agent.

CAS 211096-49-0 SB 265610

SB 265610
(CAS: 211096-49-0)

Potent CXCR2 antagonist

(CAS: 1029521-30-9)

Potent and selective CXCR2 antagonist

CAS 110078-46-1 Plerixafor

(CAS: 110078-46-1)

Plerixafor is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.

CAS 1986-81-8 Nicotinamide N-oxide

Nicotinamide N-oxide
(CAS: 1986-81-8)

Nicotinamide N-oxide, a metabolite of Nicotinamide, is a potent, and selective antagonist of the CXCR2 receptor and used in studies of mechanisms of niacin-rela...

FC 131
(CAS: 606968-52-9)

CXCR4 antagonist

CAS 956590-23-1 UNBS5162

(CAS: 956590-23-1)

A novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers

SB 332235
(CAS: 276702-15-9)

Potent CXCR2 antagonist

CAS 897657-95-3 MSX-122

(CAS: 897657-95-3)

A novel small molecule and partial CXCR4 antagonist

CAS 1204707-73-2 SRT3190

(CAS: 1204707-73-2)

A CXCR2 ligand

TC 14012
(CAS: 368874-34-4)

CXCR4 antagonist; ACKR3 (CXCR7) agonist

(CAS: 688763-64-6)

Elubrixin is a interleukin 8 inhibitor and CXCR2 selective antagonist. It is potentially useful for Inflammatory bowel disease therapies. It inhibits ex vivo ne...

CAS 1873376-49-8 CXCR2-IN-1

(CAS: 1873376-49-8)

CXCR2-IN-1 is a CXCR2 antagonists (pIC50= 9.3) with favorable central nervous system penetration property (Br/Bl>0.45).

Chemical Structure

CAS 855527-92-3 NBI-74330

Quick Inquiry

Verification code

Featured Items