Structure of PNU-282987 free base
CAS No.: 711085-63-1
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
PNU-282987 Free Base is a selective α7 nicotinic acetylcholine receptor agonist with research potential for improving cognitive function.
Synonyms: PNU 282987
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Batch number can be found on the product's label following the word 'Batch'.
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CAS No. : | 711085-63-1 |
Formula : | C14H17ClN2O |
M.W : | 264.75 |
SMILES Code : | O=C(N[C@H]1CN2CCC1CC2)C3=CC=C(Cl)C=C3 |
Synonyms : |
PNU 282987
|
MDL No. : | MFCD08703110 |
InChI Key : | WECKJONDRAUFDD-ZDUSSCGKSA-N |
Pubchem ID : | 9795278 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
Description |
PNU-282987 (free base) is a highly potent agonist of α7 nicotinic acetylcholine receptors (nAChRs), with an EC50 of 154 nM. It also functions as a functional antagonist of the 5-HT3 receptor, with an IC50 of 4541 nM. PNU-282987 (free base) is applicable in research pertaining to both the central and peripheral nervous systems [1].
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In Vitro:
Cell Line
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Concentration | Treated Time | Description | References |
bipolar cells | 30 µM | To investigate the depolarization effect of PNU-282987 on bipolar cells, results showed that type 2 and 7 bipolar cells depolarized in response to PNU application. | PMC6738513 | |
Primary mouse cortical neurons | 0.5 µM | 24 h | To evaluate the effect of PNU-282987 on Tat-induced neurotoxicity, results showed that PNU-282987 decreased PSD-95 and p-p38 expression. | PMC8677536 |
Primary mouse microglia | 0.5 µM | 24 h | To evaluate the effect of PNU-282987 on Tat-induced neurotoxicity, results showed that PNU-282987 decreased Iba-1 and p-p38 expression. | PMC8677536 |
Primary mouse astrocytes | 0.5 µM | 24 h | To evaluate the effect of PNU-282987 on Tat-induced neurotoxicity, results showed that PNU-282987 decreased GFAP and p-p38 expression. | PMC8677536 |
Primary mouse neuron-astrocyte co-cultures | 0.5 µM | 24 h | To evaluate the effect of PNU-282987 on Tat-induced neurotoxicity, results showed that PNU-282987 increased PSD-95 and p-p38 expression. | PMC8677536 |
Mouse aortic smooth muscle cells (MOVAS) | 10 μM | 24 h | Activating α7nAChR inhibited TNF-α-induced oxidative stress, NLRP3/GSDMD expression, and cell pyroptosis. | PMC9525652 |
MLE-12 cells | 30 µM | different times | PNU-282987 significantly inhibited LPS-induced MLE-12 cell injury, manifested by the increased expression of GPX4, SLC7A11 and FTH1 and the increased levels of cell viability and GSH | PMC8866566 |
BV2 microglia | 0.1, 1, and 10 µM | 12 h | To investigate the effect of PNU-282987 on autophagy in LPS-stimulated BV2 microglia. The results showed that PNU-282987 significantly enhanced the levels of autophagy-related proteins Beclin 1 and LC3-II/I ratio, and reduced the expression of p62/SQSTM1. | PMC5432615 |
Peritoneal macrophages | 30μM | Overnight | To evaluate the effect of α7nAChR deficiency on the expression of genes related to macrophage migration | PMC10765732 |
RAW264.7 cells | 5, 10, 20 μM | 4 h | To evaluate the inhibitory effect of PNU-282987 on PMA or LPS-induced histone H3 citrullination. The results showed that PNU-282987 significantly inhibited PMA and LPS-induced histone H3 citrullination. | PMC10150100 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
Mice | ApoE−/− mice | Intraperitoneal injection | 1 mg/kg | Once daily for 4 weeks | Activating α7nAChR slowed down AAA formation, reduced maximal aortic diameters, preserved elastin integrity, and inhibited inflammatory responses. | PMC9525652 |
mice | LPS-induced ALI/ARDS model | intraperitoneal injection | 5 mg/kg | single injection | LPS injection significantly induced ferroptosis events in the lung tissues of mice, manifested by elevated iron levels, ROS production and lipid peroxidation | PMC8866566 |
C57BL/6J mice | Experimental autoimmune encephalomyelitis (EAE) model | Intraperitoneal injection | 0.1 mg/kg | Once daily from day 3 until the end of the study | To investigate the alleviative effect of PNU-282987 on neuroinflammation in EAE mice. The results showed that PNU-282987 significantly ameliorated the severity of EAE and spinal inflammatory infiltration, and enhanced monocyte/microglia autophagy. | PMC5432615 |
Mice | Vascular injury model | Intraperitoneal injection | 1 mg/kg | Once daily for 4 weeks | Activation of CAP significantly reduced neointima formation, arterial inflammation and oxidative stress after vascular injury by suppressing inflammation and oxidative stress. | PMC5723281 |
Mice | db/db mouse model | Intraperitoneal injection | 10 mg/kg | Twice daily for 4 weeks | PNU-282987 exhibited a significant blood glucose-lowering effect in db/db mice, confirming its α7nAChR-mediated glucoregulatory action. | PMC9177741 |
mice | endometriosis model | osmotic pump | 2 mg/kg | once daily for 3 weeks | To evaluate the effect of PNU-282987 on the development of endometriotic lesions, results showed that PNU-282987 significantly reduced lesion weight and retarded lesional progression by hindering EMT and FMT. | PMC9166516 |
Mice | Endotoxemia model | Intraperitoneal injection | 3mg/kg | Single dose, 48 hours duration | To evaluate the effect of PNU-282987 on macrophage accumulation following α7nAChR activation | PMC10765732 |
DBA/1J mice | Collagen-induced arthritis (CIA) model | Oral | 120 mg/kg | From Day 0 to Day 21, once daily | To evaluate the effect of PNU-282987 on protein citrullination and arthritis symptoms in CIA mice. The results showed that PNU-282987 significantly reduced protein citrullination levels in ankle and splenic tissues, alleviated arthritis symptoms, and reduced bone destruction. | PMC10150100 |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.78mL 0.76mL 0.38mL |
18.89mL 3.78mL 1.89mL |
37.77mL 7.55mL 3.78mL |
Tags: PNU-282987 | PNU282987 | PNU 282987 | nAChR | 5-HT Receptor | Nicotinic acetylcholine receptors | Serotonin Receptor | 5-hydroxytryptamine Receptor | nicotinic acetylcholine receptors (nAChRs) | 5-HT3 | α7 nicotinic acetylcholine receptor | nAChR agonist | 5-HT3 receptor antagonist | 711085-63-1
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H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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