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

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

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 220 In-stock
Solution
10 mM * 1 mL in DMSO USD 220 In-stock
Solid
5 mg USD 165 In-stock
10 mg USD 275 In-stock
25 mg USD 495 In-stock
50 mg USD 935 In-stock
100 mg USD 1485 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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]

[125I]CXCL10-CXCR3

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

[125I]CXCL11-CXCR3

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].

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

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].

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

Molecular Weight

605.58

Formula

C32H27F4N5O3

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N([C@@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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (165.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (4.13 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.13 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Kinase Assay
[1]

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
[3]

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.

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6513 mL 8.2565 mL 16.5131 mL 41.2827 mL
5 mM 0.3303 mL 1.6513 mL 3.3026 mL 8.2565 mL
10 mM 0.1651 mL 0.8257 mL 1.6513 mL 4.1283 mL
15 mM 0.1101 mL 0.5504 mL 1.1009 mL 2.7522 mL
20 mM 0.0826 mL 0.4128 mL 0.8257 mL 2.0641 mL
25 mM 0.0661 mL 0.3303 mL 0.6605 mL 1.6513 mL
30 mM 0.0550 mL 0.2752 mL 0.5504 mL 1.3761 mL
40 mM 0.0413 mL 0.2064 mL 0.4128 mL 1.0321 mL
50 mM 0.0330 mL 0.1651 mL 0.3303 mL 0.8257 mL
60 mM 0.0275 mL 0.1376 mL 0.2752 mL 0.6880 mL
80 mM 0.0206 mL 0.1032 mL 0.2064 mL 0.5160 mL
100 mM 0.0165 mL 0.0826 mL 0.1651 mL 0.4128 mL
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NBI-74330 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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