BPN-37440
BPN-37440 is a blood-brain barrier-permeable, selective, and orally active EP2 receptor inhibitor with an IC50 of 53-60 nM. BPN-37440 inhibits the expression of inflammatory mediators IL-1β and COX-2, with an IC50 of 21 nM for IL-1β and 42 nM for COX-2. BPN-37440 reduces microgliosis in key brain regions of mice with pilocarpine (HY-B0726A)-induced status epilepticus and reverses their working memory and recognition memory deficits. BPN-37440 can be used for research on status epilepticus.
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- CAS. Nr.: 3120759-70-5
- Formel: C21H22N4O
- Molecular Weight:346.43
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
EP2 53-60 nM (IC50) |
IL-1β 21 nM (IC50) |
COX-2 42 nM (IC50) |
In Vitro
BPN-37440 (0.01-10000 nM) potently and selectively inhibits the EP2 receptor in C6 glioma cells, with an IC50 of 53-60 nM[1].
BPN-37440 (30-1000 nM) acts as an inhibitor of the hEP2 receptor (KB = 5.65 nM) and mouse EP2 receptor (KB = 9.55 nM) in C6 glioma cells[1].
BPN-37440 (0-1000 nM; 30 min preincubation, 2 h stimulation) potently inhibits the expression of inflammatory mediators induced by LPS/EP2 agonists in BV2-hEP2 microglia, with an IC50 of 21 nM for IL-1β and 42 nM for COX-2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BV2 microglial cells overexpressing human EP2 receptors (BV2-hEP2)
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Concentration:0-1000 nM
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Incubation Time:30 min (preincubation); 2 h (stimulation)
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Result:Significantly attenuated the LPS/CP544326-induced upregulation of COX-2, IL-6, and IL-1β mRNA in a concentration-dependent manner.
Inhibited IL-1β induction with an IC50 of 21 nM.
Inhibited COX-2 induction with an IC50 of 42 nM.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 8-12 weeks old)[1]
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Dosage:10 mg/kg
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Administration:i.p.; 3 times (3-4, 6-8, and 19 hours after SE onset)
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Result:Regained weight faster than vehicle-treated SE mice, with significant difference in weight loss on day 2 post-SE (P = 0.0043).
Attenuated microgliosis (measured by IBA 1 positive area covered) in the amygdala (P = 0.0130), cortex (P = 0.0038), and hippocampus CA3 region (P = 0.0183) 4 days post-SE; showed a reducing trend in the hippocampus CA1 region.
Reduced SE-induced increases in hippocampal inflammatory mediator mRNA levels (P = 0.033).
Improved working memory, with an alternation index of 0.65 compared to 0.54 in vehicle-treated SE mice (P = 0.033); no impact on distance traveled in the Y-maze.
Restored recognition memory, with a discrimination index of 0.277 in the novel object recognition test (P < 0.0001), compared to 0.048 in vehicle-treated SE mice.
Chemical Information
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CAS. Nr. 3120759-70-5
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Molecular Weight 346.43
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Formel C21H22N4O
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SMILES
O=C(C1=CC2=C(C(C)=NC=C2)N1C)NCCC3=C(C)NC4=CC=CC=C43
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
BPN-37440 Related Classifications
HY-183149 Related Classifications
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