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Chemical Structure| 711085-63-1 Chemical Structure| 711085-63-1

Structure of PNU-282987 free base
CAS No.: 711085-63-1

Chemical Structure| 711085-63-1

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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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Product Details of PNU-282987 free base

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

Safety of PNU-282987 free base

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of PNU-282987 free base

GPCR

Isoform Comparison

Biological Activity

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].

In Vitro:

Cell Line
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

Protocol

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

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