2. GPCR/G Protein Immunology/Inflammation
  3. Prostaglandin Receptor Interleukin Related COX
  4. 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.

For research use only. We do not sell to patients.

BPN-37440

BPN-37440 Chemical Structure

CAS No. : 3120759-70-5

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BPN-37440 Related Antibodies

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Description

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[1].

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.

BPN-37440 Related Antibodies

Real Time qPCR[1]

Cell Line: BV2 microglial cells overexpressing human EP2 receptors (BV2-hEP2)
Concentration: 0-1000 nM
Incubation Time: 30 min (preincubation); 2 h (stimulation)
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
Species Dose Route Tmax (Plasma) AUClast AUCinf T1/2 MRTlast F CL
Rat[1] 10 mg/kg p.o. 0.5 h 3786 ng·h/mL 3791 ng·h/mL 0.76 h 1.78 h 88 % /
Rat[1] 2 mg/kg i.v. / 865 ng·h/mL 876 ng·h/mL 1.86 h 0.8 h / 38.0 mL/min/kg
In Vivo

BPN-37440 (10 mg/kg; i.p.; 3 administrations) reduces microglial proliferation in key brain regions of mice with pilocarpine (HY-B0726A)-induced status epilepticus, and reverses their working memory and recognition memory deficits[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (male, 8-12 weeks old)[1]
Dosage: 10 mg/kg
Administration: i.p.; 3 times (3-4, 6-8, and 19 hours after SE onset)
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.
Molecular Weight

346.43

Formula

C21H22N4O
CAS No.
SMILES

O=C(C1=CC2=C(C(C)=NC=C2)N1C)NCCC3=C(C)NC4=CC=CC=C43
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BPN-37440 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BPN-374403120759-70-5BPN37440BPN 37440Prostaglandin ReceptorInterleukin RelatedCOXILCyclooxygenaseEP4 receptorCYP2C8IP prostanoid receptorC6-glioma cellsDP1 receptorBV2-hEP2 microglial cellsstatus epilepticusEP2 receptorCYP3A4MDR1-MDCK cellsInhibitorinhibitorinhibit

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