PD 144795
PD 144795 is an orally active inhibitor of E-selectin (E-selectin), ICAM-1, and VCAM-1, with IC50 values of 6.6 μM, 4.0-10 μM, and 4.0 μM for the human targets, respectively. PD 144795 has favorable pharmacokinetic properties, including good absorption and no endothelial cytotoxicity. PD 144795 inhibits TNF-α-induced adhesion of neutrophils and monocytes to endothelial cells, reduces neutrophil infiltration, exudate accumulation, and footpad swelling, and delays disease progression in rodent models. PD 144795 can be used for inflammation-related research.
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- CAS No.: 148550-96-3
- Formule: C13H15NO4S
- Masse moléculaire:281.33
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HUVEC | IC50 |
8.7 μM
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Inhibition of TNF-α-stimulated neutrophil adhesion to human umbilical vein endothelial cells (HUVECs) measured via γ-ray spectroscopy after 4h incubation with TNF-α and 30min neutrophil incubation.
Inhibition of TNF-α-stimulated neutrophil adhesion to human umbilical vein endothelial cells (HUVECs) measured via γ-ray spectroscopy after 4h incubation with TNF-α and 30min neutrophil incubation.
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jm00022a026 |
| HUVEC | IC50 |
4.0 μM
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Inhibition of TNF-α-induced ICAM-1 surface expression on human umbilical vein endothelial cells (HUVECs) measured via ELISA after 30min pre-incubation with test compound followed by 4h TNF-α stimulation.
Inhibition of TNF-α-induced ICAM-1 surface expression on human umbilical vein endothelial cells (HUVECs) measured via ELISA after 30min pre-incubation with test compound followed by 4h TNF-α stimulation.
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jm00022a026 |
| HUVEC | IC50 |
6.6 μM
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Inhibition of TNF-α-induced E-selectin surface expression on human umbilical vein endothelial cells (HUVECs) measured via ELISA after 30min pre-incubation with test compound followed by 4h TNF-α stimulation.
Inhibition of TNF-α-induced E-selectin surface expression on human umbilical vein endothelial cells (HUVECs) measured via ELISA after 30min pre-incubation with test compound followed by 4h TNF-α stimulation.
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jm00022a026 |
| HUVEC | IC50 |
5.7 μM
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Inhibition of TNF-α-induced ICAM-1 surface expression on human umbilical vein endothelial cells (HUVECs) by the S-enantiomer of PD 144795 measured via ELISA.
Inhibition of TNF-α-induced ICAM-1 surface expression on human umbilical vein endothelial cells (HUVECs) by the S-enantiomer of PD 144795 measured via ELISA.
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jm00022a026 |
| HUVEC | IC50 |
9.6 μM
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Inhibition of TNF-α-induced E-selectin surface expression on human umbilical vein endothelial cells (HUVECs) by the S-enantiomer of PD 144795 measured via ELISA.
Inhibition of TNF-α-induced E-selectin surface expression on human umbilical vein endothelial cells (HUVECs) by the S-enantiomer of PD 144795 measured via ELISA.
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jm00022a026 |
In Vitro
PD 144795 (pretreatment for 30 minutes + incubation for 4 hours) inhibits TNF-α-induced expression of ICAM-1 and E-selectin on the surface of human umbilical vein endothelial cells, with IC50 values of 4.0 μM and 6.6 μM, respectively[1].
PD 144795 (overnight treatment) inhibits the adhesion of U937 monocytes to human aortic endothelial cells under TNF-α stimulation, with an IC50 of 8.8 μM[1].
PD 144795 (incubated for 18 h) inhibits TNF-α-induced expression of VCAM-1 and ICAM-1 on the surface of human aortic endothelial cells, with IC50 values of 4.0 μM and 10 μM, respectively[1].
PD 144795 modulates the expression of TNF-α-responsive genes in human umbilical vein endothelial cells and human aortic endothelial cells without inhibiting NF-κB activation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PD 144795 (10 mg/kg; p.o.; single dose 1 hour prior to challenge) inhibits neutrophil accumulation by 68% and pleural exudate volume by 93% in a rat reverse passive Arthus pleurisy model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c (female, inbred)[1]
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Dosage:63 mg/kg (ID50)
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Administration:p.o.
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Result:Achieved an ID50 of 63 mg/kg for inhibiting neutrophil influx into the peritoneal cavity.
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Animal Model:Wistar (male, outbred, 220-245 g)[1]
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Dosage:10 mg/kg
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Administration:p.o.; single dose 1 hour prior to challenge
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Result:Inhibited neutrophil accumulation by 68%.
Inhibited pleural exudate volume by 93%.
Chemical Information
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CAS No. 148550-96-3
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Masse moléculaire 281.33
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Formule C13H15NO4S
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SMILES
O=C(N)C1=C(OC(C)C)C=2C=C(OC)C=CC2S1=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PD 144795 Related Classifications
HY-187620 Related Classifications
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