RWJ 50271
Based on 1 Customer Validation
RWJ 50271 is an selective and orally active inhibitor of lymphocyte function-associated antigen-1/intercellular adhesion molecule-1(LFA-1/ICAM-1) interaction with an IC50 of 5.0 μM (HL60 cells). RWJ 50271 inhibits LFA-1/ICAM-1-mediated cell adhesion.
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- Purity: 99.23%
- CAS No.: 162112-37-0
- 화학식: C18H17F3N4O2S
- 분자량:410.41
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보관: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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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
IC50: 5.0 μM (LFA-1/ICAM-1, HL60 cells)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
5 μM
Compound: 4
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Inhibition of HL-60 cell adhesion to purified ICAM-1 by LFA-1
Inhibition of HL-60 cell adhesion to purified ICAM-1 by LFA-1
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[PMID: 7707308] |
| HL-60 | IC50 |
5 μM
Compound: 4
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The concentration of compound required to inhibit 50% interaction (IC50 ) was measured on LFA-1/ICAM-1 mediated cells using cell/cell adherence assay on the HL60/U937 test system
The concentration of compound required to inhibit 50% interaction (IC50 ) was measured on LFA-1/ICAM-1 mediated cells using cell/cell adherence assay on the HL60/U937 test system
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[PMID: 7707308] |
| HL-60 | IC50 |
5 μM
Compound: 4
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Inhibition of LFA-1 mediated HL60 cell adhesion to ICAM-1
Inhibition of LFA-1 mediated HL60 cell adhesion to ICAM-1
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[PMID: 7707308] |
In Vitro
RWJ 50271 inhibits adhesion of peripheral blood lymphocytes to plastic immobilized SICAM-1[1].
RWJ 50271 inhibits both human and murine NK activity (IC50=5.0 μM) in an LFA-1/ICAM-1-dependent natural killer [NK] cytotoxicity assay[1].
RWJ 50271 does not inhibit Mac-1/ICAM-1, E-selectidsialyl Lewis X or VLA-4/VCAM-1-mediated cell adhesion up to 20 μM concentrations[1].
RWJ 50271 does not alter the LFA-1 expression levels on HL60 cells[1].
RWJ 50271 inhibits adhesion of peripheral blood lymphocytes to plastic immobilized SICAM-1[1].
RWJ 50271 does not exhibit any toxic activity up to 100 μM concentrations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice, the delayed-type hypersensitivity [DTH] reaction model[1]
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Dosage:50 mg/kg
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Administration:Oral administration
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Result:Significantly reduced foot pad swelling (>50%) 48 h after the challenge.
Chemical Information
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CAS No. 162112-37-0
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Appearance Solid
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분자량 410.41
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화학식 C18H17F3N4O2S
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Color White to off-white
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SMILES
CC1=C(C(NCCCO)=O)C=NN1C2=NC(C3=CC(C(F)(F)F)=CC=C3)=CS2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 250 mg/mL (609.15 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: ≥ 2.08 mg/mL (5.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
순도&문서
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Data Sheet (270 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 | 2.4366 mL | 12.1829 mL | 24.3659 mL | 60.9147 mL |
| 5 mM | 0.4873 mL | 2.4366 mL | 4.8732 mL | 12.1829 mL | |
| 10 mM | 0.2437 mL | 1.2183 mL | 2.4366 mL | 6.0915 mL | |
| 15 mM | 0.1624 mL | 0.8122 mL | 1.6244 mL | 4.0610 mL | |
| 20 mM | 0.1218 mL | 0.6091 mL | 1.2183 mL | 3.0457 mL | |
| 25 mM | 0.0975 mL | 0.4873 mL | 0.9746 mL | 2.4366 mL | |
| 30 mM | 0.0812 mL | 0.4061 mL | 0.8122 mL | 2.0305 mL | |
| 40 mM | 0.0609 mL | 0.3046 mL | 0.6091 mL | 1.5229 mL | |
| 50 mM | 0.0487 mL | 0.2437 mL | 0.4873 mL | 1.2183 mL | |
| 60 mM | 0.0406 mL | 0.2030 mL | 0.4061 mL | 1.0152 mL | |
| 80 mM | 0.0305 mL | 0.1523 mL | 0.3046 mL | 0.7614 mL | |
| 100 mM | 0.0244 mL | 0.1218 mL | 0.2437 mL | 0.6091 mL |
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