1. GPCR/G Protein
  2. CXCR
  3. NBI-74330


Cat. No.: HY-15320 Purity: 99.23%
Handling Instructions

NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of (125I)CXCL10 and (125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively.

For research use only. We do not sell to patients.

NBI-74330 Chemical Structure

NBI-74330 Chemical Structure

CAS No. : 855527-92-3

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1  mL in DMSO USD 200 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
25 mg USD 450 In-stock
Estimated Time of Arrival: December 31
50 mg USD 850 In-stock
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100 mg USD 1350 In-stock
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NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of (125I)CXCL10 and (125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively.

IC50 & Target[1]


1.5 nM (Ki, in CXCR3-CHO cell membranes)


3.2 nM (Ki, in CXCR3-CHO cell membranes)

In Vitro

BI-74330 demonstrates potent inhibition of [125I]CXCL11 specific binding to membranes prepared from transfected CHO cells expressing CXCR3 (CXCR3-CHO) (Ki=3.6 nM). NBI-74330 is 12- and 3.5-fold more potent than CXCL9 (Ki=45.2 nM) and CXCL10 (Ki=12.5 nM), respectively, at inhibiting [125I]CXCL11 binding to CXCR3-CHO cell membranes. NBI-74330 inhibits calcium mobilization in response to CXCL11 and CXCL10 with an IC50 value of 7 nM for both ligands used at their EC80 concentrations (1 nM for CXCL11 and 30 nM for CXCL10). NBI-74330 specifically inhibits CXCR3-mediated calcium mobilization. NBI-74330 also dose-dependently inhibits CXCL11-induced [35S]GTPγS binding in membranes of cells endogenously expressing CXCR3 (H9 cells, IC50 value 5.5 nM). BI-74330 inhibits CXCL11-induced chemotaxis in these cells with an IC50 of 3.9 nM[1]. NBI-74330 (30-300 nm, 1-10 μM) produces concentration-dependent, parallel rightward shifts of the CXCL11 E/[A] curve with no significant change in the E/[A] curve maximal response[2].

In Vivo

NBI-74330 (100 mg/kg) results in the formation of an N-oxide metabolite, also an antagonist of CXCR3, in mice[2]. Mice treated with 100 mg/kg NBI-74330 (in 1% Na Doc in 0.5% 400Cp Methylcellulose) result in serum concentrations of approximately 1 μM. This concentration is sufficient to fully block the CXCR3 receptor in vivo[3].

Molecular Weight







O=C(N([[email protected]@H](C1=NC2=NC=CC=C2C(N1C3=CC=C(OCC)C=C3)=O)C)CC4=CC=CN=C4)CC5=CC=C(F)C(C(F)(F)F)=C5


Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 35 mg/mL (57.80 mM)

*"≥" means soluble, but saturation unknown.

Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6513 mL 8.2565 mL 16.5131 mL
5 mM 0.3303 mL 1.6513 mL 3.3026 mL
10 mM 0.1651 mL 0.8257 mL 1.6513 mL
*Please refer to the solubility information to select the appropriate solvent.
Kinase Assay

Cell membrane fractions are resuspended in 50 mM HEPES, 10 mM MgCl2, 100 mM NaCl, and 1 mM CaCl2, pH 7.2 for use in competitive radioligand binding reactions. Reactions are performed in duplicate and consisted of 25-μL unlabeled chemokine at indicated concentrations, 25-μL radiolabeled chemokine ligand (appr 70 nM; [125I]CXCL11 and [125I]CXCL10 with specific activities of 1500 and 2200 Ci/mmol, respectively; Fifty-μL membrane protein (5 μg) are added sequentially in assay buffer (50 mM HEPES, 10 mM MgCl2, 100 mM NaCl, 1 mM CaCl2, and 0.1% BSA, pH 7.2) to low-binding 96-well plates. The reaction is allowed to reach equilibrium by incubation at room temperature for 45 min while shaking. The amount of bound radioligand is determined by harvesting membranes via filtration through a UniFilter GF/C filter plate using a UniFilter-96 vacuum manifold (filters are pretreated with 1% polyethylenimine), washing twice with 400-μL wash buffer (10 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, and 500 mM NaCl, pH 7.3), and measuring radioactivity by liquid scintillation using a TopCount NXT. The dissociation half-life of [125I]CXCL11 is measured using CXCR3-CHO membranes that are allowed to equilibrate with radiolabel (appr 70 nM) for 30 min prior to the addition of excess cold CXCL11 (31 nM final) in the presence or absence of different concentrations of NBI-74330. Membrane-bound [125I]CXCL11 is assessed in duplicate along with nonspecific binding ([125I]CXCL11 plus excess cold CXCL11 added at the same) and total binding ([125I]CXCL11 without inhibitors) at each time point on the same plate.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration

Female LDLr−/− mice, 10 weeks old (n=8 to 12 per group), are fed a Western-type diet containing 0.25% cholesterol and 15% cocoa butter 2 weeks before collar placement. 20 Mice are treated with a subcutaneous injection of 100 mg/kg NBI-74330 every day during the entire experiment. After 8 weeks of Western-type diet and treatment, the mice are euthanized and organs are harvested for histology, fluorescence-activated-cell sorter (FACS) analysis, and RNA isolation. Blood samples are collected by tail bleeding from nonfasted animals, and concentrations of serum cholesterol and triglycerides are determined using enzymatic colorimetric procedures.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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NBI-74330NBI74330NBI 74330CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsInhibitorinhibitorinhibit

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