CXCR3 antagonist 1
Based on 1 Customer Validation
CXCR3 antagonist 1 (compound 6c) is a selective and non-cytotoxic CXCR3 antagonist (IC50=0.06 µM). CXCR3 antagonist 1 has potential in researching inflammatory diseases (including inflammatory bowel disease, multiple sclerosis, rheumatoid arthritis, and diabetes).
For research use only. We do not sell to patients.
- Purity : 98.6%
- CAS No.: 870998-13-3
- Formula: C30H32Cl3N5O3
- Molecular Weight:616.97
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Description
IC50 & Target
[1]|
CXCR3 0.06 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.06 μM
Compound: 6c
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Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
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[PMID: 16213722] |
| HEK293 | IC50 |
20 nM
Compound: 6c
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Inhibition of CXCL10 (IP-10)-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
Inhibition of CXCL10 (IP-10)-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
|
[PMID: 16213722] |
Chemical Information
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CAS No. 870998-13-3
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Appearance Solid
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Molecular Weight 616.97
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Formula C30H32Cl3N5O3
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Color White to off-white
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SMILES
O=C(C1=CC(Cl)=CC=C1)NC2=CC(C(NCCC3=CC=C(C=C3Cl)Cl)=O)=CC=C2N4CCN(CCC4)C(NCC)=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 : 50 mg/mL (81.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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: ≥ 1.25 mg/mL (2.03 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
Purity & Documentation
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Data Sheet (271 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6208 mL | 8.1041 mL | 16.2082 mL | 40.5206 mL |
| 5 mM | 0.3242 mL | 1.6208 mL | 3.2416 mL | 8.1041 mL | |
| 10 mM | 0.1621 mL | 0.8104 mL | 1.6208 mL | 4.0521 mL | |
| 15 mM | 0.1081 mL | 0.5403 mL | 1.0805 mL | 2.7014 mL | |
| 20 mM | 0.0810 mL | 0.4052 mL | 0.8104 mL | 2.0260 mL | |
| 25 mM | 0.0648 mL | 0.3242 mL | 0.6483 mL | 1.6208 mL | |
| 30 mM | 0.0540 mL | 0.2701 mL | 0.5403 mL | 1.3507 mL | |
| 40 mM | 0.0405 mL | 0.2026 mL | 0.4052 mL | 1.0130 mL | |
| 50 mM | 0.0324 mL | 0.1621 mL | 0.3242 mL | 0.8104 mL | |
| 60 mM | 0.0270 mL | 0.1351 mL | 0.2701 mL | 0.6753 mL | |
| 80 mM | 0.0203 mL | 0.1013 mL | 0.2026 mL | 0.5065 mL |