2. GPCR/G Protein Immunology/Inflammation
  3. CXCR
  4. YU241279

YU241279 is an orally active CXCR5 inhibitor. YU241279 inhibits CXCL13-mediated Gαq-dependent calcium influx and Gαi2-dependent cAMP reduction in CXCR5-expressing cells. YU241279 inhibits the proliferation of CXCR5-expressing lymphoma cells. YU241279 reduces tumor burden in the peripheral blood and bone marrow of mice implanted with lymphoma tissues. YU241279 is well tolerated during oral administration in mice, maintains stable plasma drug concentrations, and shows no metabolic changes. YU241279 can be used in the research of angioimmunoblastic T-cell lymphoma and Burkitt B-cell lymphoma.

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YU241279

YU241279 Chemical Structure

CAS No. : 1092445-63-0

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Based on 1 publication(s) in Google Scholar

YU241279 Related Antibodies

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Description

YU241279 is an orally active CXCR5 inhibitor. YU241279 inhibits CXCL13-mediated Gαq-dependent calcium influx and Gαi2-dependent cAMP reduction in CXCR5-expressing cells. YU241279 inhibits the proliferation of CXCR5-expressing lymphoma cells. YU241279 reduces tumor burden in the peripheral blood and bone marrow of mice implanted with lymphoma tissues. YU241279 is well tolerated during oral administration in mice, maintains stable plasma drug concentrations, and shows no metabolic changes. YU241279 can be used in the research of angioimmunoblastic T-cell lymphoma and Burkitt B-cell lymphoma[1].

In Vitro

YU241279 (compound 2) potently inhibits Gaq-mediated Ca2+ flux in division-arrested HEK-293 cells stably expressing human CXCR5, with IC50 values of 166.4 nM in HBSS buffer and 444.4 nM in HBSS buffer + 1% BSA[1].
YU241279 potently inhibits Gαi2-mediated cAMP decrease in division-arrested HEK-293 cells stably expressing human CXCR5, with IC50 values of 341.1 nM in HBSS buffer and 584.5 nM in HBSS buffer + 1% BSA[1].
YU241279 (1-30 μM; 7 days) dose-dependently inhibits proliferation of CXCR5-expressing Raji Burkitt's B-cell lymphoma cells[1].

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

YU241279 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: CXCR5-expressing Raji Burkitt's B-cell lymphoma cells
Concentration: 1-30 μM
Incubation Time: 7 days
Result: Induced a dose-dependent decrease in Raji cell proliferation over 7 days.
Significantly reduced proliferation relative to DMSO control at 1 μM (p<0.01).
Significantly reduced proliferation relative to DMSO control at 3 μM, 10 μM, and 30 μM (p<0.005 for each).
In Vivo

YU241279 (compound 2) (40 mg/kg; oral gavage; twice daily; 42 days) produces a significant reduction in AITL tumor burden in NSG mice[1].

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

Animal Model: NSG (NOD/SCID, IL-2R knockout; 8 animals per group)[1]
Dosage: 40 mg/kg
Administration: oral gavage; twice daily; 42 days
Result: Reduced absolute percentage of human CD45+ cells in bone marrow to 10.6%.
Reduced absolute percentage of human CD45+ cells in peripheral blood to 44.5%.
Maintained 5 surviving mice at study end.
Molecular Weight

351.44

Formula

C22H25NO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1(CC2=C(C1)C=CC=C2)NC(C3=CC=CC(C)=C3CC(C)C)=O)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (284.54 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8454 mL 14.2272 mL 28.4544 mL
5 mM 0.5691 mL 2.8454 mL 5.6909 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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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 (7.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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% Corn Oil

    Solubility: 2.5 mg/mL (7.11 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 Corn oil, and mix evenly.

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

Dosage

mg/kg

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(per animal)

g

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(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

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8454 mL 14.2272 mL 28.4544 mL 71.1359 mL
5 mM 0.5691 mL 2.8454 mL 5.6909 mL 14.2272 mL
10 mM 0.2845 mL 1.4227 mL 2.8454 mL 7.1136 mL
15 mM 0.1897 mL 0.9485 mL 1.8970 mL 4.7424 mL
20 mM 0.1423 mL 0.7114 mL 1.4227 mL 3.5568 mL
25 mM 0.1138 mL 0.5691 mL 1.1382 mL 2.8454 mL
30 mM 0.0948 mL 0.4742 mL 0.9485 mL 2.3712 mL
40 mM 0.0711 mL 0.3557 mL 0.7114 mL 1.7784 mL
50 mM 0.0569 mL 0.2845 mL 0.5691 mL 1.4227 mL
60 mM 0.0474 mL 0.2371 mL 0.4742 mL 1.1856 mL
80 mM 0.0356 mL 0.1778 mL 0.3557 mL 0.8892 mL
100 mM 0.0285 mL 0.1423 mL 0.2845 mL 0.7114 mL
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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.

Keywords:

YU2412791092445-63-0YU 241279YU-241279CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsangioimmunoblastic T cell lymphomaBurkitt's B-cell lymphomaCXCR5-expressing cellsGaqGai2miceHEK-293 cellslymphoma cellsCXCR5CXCL13Inhibitorinhibitorinhibit

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