YU241279
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity : 99.58%
- CAS No.: 1092445-63-0
- Formula: C22H25NO3
- Molecular Weight:351.44
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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. Further protocols information, click here.
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Cell Line:CXCR5-expressing Raji Burkitt's B-cell lymphoma cells
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Concentration:1-30 μM
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Incubation Time:7 days
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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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG (NOD/SCID, IL-2R knockout; 8 animals per group)[1]
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Dosage:40 mg/kg
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Administration:oral gavage; twice daily; 42 days
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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.
Chemical Information
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CAS No. 1092445-63-0
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Appearance Solid
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Molecular Weight 351.44
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Formula C22H25NO3
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Color White to off-white
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SMILES
O=C(C1(CC2=C(C1)C=CC=C2)NC(C3=CC=CC(C)=C3CC(C)C)=O)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocols
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How to Select the Route of Administration for Mammals
Route-of-administration selection in mammals is a pharmacokinetic, pharmacodynamic, formulation, animal-welfare, and translational decision, not a default technical choice. The selected route should match the study goal: intravenous dosing is most useful when complete systemic exposure and rapid onset are required, oral dosing is most translational for orally intended medicines but is affected by absorption and first-pass metabolism, subcutaneous or intramuscular dosing can provide slower systemic exposure, and intraperitoneal dosing can be useful in rodent proof-of-concept studies but may have limited clinical translation. Published route-comparison studies show that the same compound can produce different exposure, onset, bioavailability, tissue distribution, and tolerability depending on route; therefore, route choice should be supported by pilot pharmacokinetic or pharmacodynamic evidence when the literature is insufficient. Unresolved questions include how to standardize route sel
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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 |
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| 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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