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

(±)-NBI-74330 is a potent and selective CXCR3 antagonist. (±)-NBI-74330 not only reduces tactile and thermal hypersensitivity but also enhances the analgesic properties of morphine. (±)-NBI-74330 can reduce microglial cell activation, increase astroglial cell activation, and downregulate the expression of some CXCR3 ligands in a rat neuropathic pain model.

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(±)-NBI-74330 Chemical Structure

(±)-NBI-74330 Chemical Structure

CAS No. : 473722-68-8

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Description

(±)-NBI-74330 is a potent and selective CXCR3 antagonist. (±)-NBI-74330 not only reduces tactile and thermal hypersensitivity but also enhances the analgesic properties of morphine. (±)-NBI-74330 can reduce microglial cell activation, increase astroglial cell activation, and downregulate the expression of some CXCR3 ligands in a rat neuropathic pain model[1].

Molecular Weight

605.58

Formula

C32H27F4N5O3

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=C(N=C(C(C)N(CC3=CC=CN=C3)C(CC4=CC=C(C(C(F)(F)F)=C4)F)=O)N1C5=CC=C(C=C5)OCC)N=CC=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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
  • Molarity Calculator

  • Dilution Calculator

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

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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.13 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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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

Complete Stock Solution Preparation Table

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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(±)-NBI-74330
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