KF38789
Based on 2 publication(s) in Google Scholar
KF38789 is a selective inhibitor of P-selectin-PSGL-1 binding. KF38789 inhibits the binding of U937 cells to immobilized P-selectin immunoglobulin G chimeric protein (P-selectin-Ig) with an IC50 value of 1.97 μM.
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- Pureza: 99.56%
- No. CAS: 257292-29-8
- Fòrmula: C19H21NO5S
- Peso molecular:375.44
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) KF38789
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | EC50 |
0.56 μM
Compound: 5c
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Induction of apoptosis in human HCT116 cells assessed as caspase activation after 24 hrs by HTS assay
Induction of apoptosis in human HCT116 cells assessed as caspase activation after 24 hrs by HTS assay
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[PMID: 17562361] |
| HCT-116 | GI50 |
0.25 μM
Compound: 5c
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Growth inhibition of human HCT116 cells after 48 hrs
Growth inhibition of human HCT116 cells after 48 hrs
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[PMID: 17562361] |
| T47D | EC50 |
0.41 μM
Compound: 5c
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Induction of apoptosis in human T47D cells assessed as caspase activation after 24 hrs by HTS assay
Induction of apoptosis in human T47D cells assessed as caspase activation after 24 hrs by HTS assay
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[PMID: 17562361] |
| T47D | GI50 |
0.21 μM
Compound: 5c
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Growth inhibition of human T47D cells after 48 hrs
Growth inhibition of human T47D cells after 48 hrs
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[PMID: 17562361] |
In Vitro
KF38789 inhibits P-selectin-induced superoxide production from human polymorphonuclear cells. Intravenously injected KF38789 significantly inhibits the thioglycollate (TG)-induced accumulation of leukocytes in the mouse peritoneal cavity[1].
KF38789 displays a concentration-dependent inhibition of U937 cell adhesion to immobilized P-selectin-Ig with an IC50 value of 1.97±0.74 μM[1].
KF38789 specifically inhibits P-selectin-dependent cell adhesion and the leukocyte recruitment in mouse peritonitis[1].
KF38789 (5 μM) significantly reduces closure of a 500-μm gap between confluent sheets of Human corneal epithelial (HCE)-T cells over an 8-hr period (by ～40%)[2].
Corneal epithelial cell migration is reduced in the presence of KF38789 (5 μM) [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Intraperitoneal injection of the P-selectin inhibitor KF38789 (daily intraperitoneal injection of 10mg/kg for 12 days) significantly reduces mechanical allodynia in the facial carrageenan-injected mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice[1]
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Dosage:1 mg/kg
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Administration:Intravenously administrated
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Result:Significantly reduced leukocyte accumulation.
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Animal Model:Twenty-four adult male C57BL/6J (B6) mice, about 6-8 weeks of age and weighing approximately 20-30 g[3]
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Dosage:10 mg/kg, 1 mg/kg, 0.1 mg/kg, 0.01 mg/kg or 0.001 mg/kg
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Administration:Intraperitoneal injection daily for 12 days
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Result:Significantly reduced mechanical allodynia in the facial carrageenan-injected mice.
Chemical Information
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No. CAS 257292-29-8
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Appearance Solid
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Peso molecular 375.44
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Fòrmula C19H21NO5S
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Color Light yellow to yellow
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SMILES
O=C1OC(C)=CC(O)=C1C2=NCCSC(C2)C3=CC=C(C=C3OC)OC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
In Vitro:
DMSO : 25 mg/mL (66.59 mM; ultrasonic and warming and heat to 60°C; 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: ≥ 2.5 mg/mL (6.66 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.66 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. S Ohta, et al. Inhibition of P-selectin specific cell adhesion by a low molecular weight, non-carbohydrate compound, KF38789. Inflamm Res. 2001 Nov;50(11):544-51. [Content Brief]
[2]. Peter J Gillies, et al. Demonstration of P-selectin expression and potential function in human corneal epithelial cells. Exp Eye Res. 2018 Nov;176:196-206. [Content Brief]
[3]. Kay-Wee Poh, et al. Global gene expression analysis in the mouse brainstem after hyperalgesia induced by facial carrageenan injection--evidence for a form of neurovascular coupling? Pain. 2009 Mar;142(1-2):133-41. [Content Brief]
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 | 2.6635 mL | 13.3177 mL | 26.6354 mL | 66.5885 mL |
| 5 mM | 0.5327 mL | 2.6635 mL | 5.3271 mL | 13.3177 mL | |
| 10 mM | 0.2664 mL | 1.3318 mL | 2.6635 mL | 6.6589 mL | |
| 15 mM | 0.1776 mL | 0.8878 mL | 1.7757 mL | 4.4392 mL | |
| 20 mM | 0.1332 mL | 0.6659 mL | 1.3318 mL | 3.3294 mL | |
| 25 mM | 0.1065 mL | 0.5327 mL | 1.0654 mL | 2.6635 mL | |
| 30 mM | 0.0888 mL | 0.4439 mL | 0.8878 mL | 2.2196 mL | |
| 40 mM | 0.0666 mL | 0.3329 mL | 0.6659 mL | 1.6647 mL | |
| 50 mM | 0.0533 mL | 0.2664 mL | 0.5327 mL | 1.3318 mL | |
| 60 mM | 0.0444 mL | 0.2220 mL | 0.4439 mL | 1.1098 mL |
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