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Chemical Structure| 123464-89-1 Chemical Structure| 123464-89-1

Structure of PNU-282987
CAS No.: 123464-89-1

Chemical Structure| 123464-89-1

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PNU-282987 is a selective α7 nAChR agonist with ki value of 26nM and displays almost no effect on α1β1γδ and α3β4 nAChRs.

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Product Details of PNU-282987

CAS No. :123464-89-1
Formula : C14H18Cl2N2O
M.W : 301.21
SMILES Code : O=C(N[C@H]1CN2CCC1CC2)C3=CC=C(Cl)C=C3.[H]Cl
MDL No. :MFCD08703110

Safety of PNU-282987

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

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Mouse aortic smooth muscle cells (MOVAS) 10 μM 1 h Activating α7nAChR inhibited TNF-α-induced oxidative stress, NLRP3 inflammasome activation, and cell pyroptosis. PMC9525652

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Perforation model of subarachnoid hemorrhage Intraperitoneal injection 12mg/kg or 4mg/kg Single dose, 1 hour after surgery To evaluate whether PNU-282987 attenuates early brain injury after SAH and whether α7nAChR stimulation is associated with down regulation of caspase activity via PI3K-Akt signaling. Results showed that PNU-282987 improved neurological deficits both 24 and 72 hours after surgery and reduced brain water content in left hemispheres 24 hours after surgery. PNU-282987 significantly increased p-Akt levels and significantly decreased CC3 levels in ipsilateral hemispheres after SAH. PMC3226904
Mice Vascular injury model Intraperitoneal injection 1 mg/kg Once daily for 4 weeks PNU-282987 significantly reduced neointima formation, arterial inflammation and oxidative stress after vascular injury PMC5723281
Mice Intracerebral hemorrhage model Intraperitoneal injection 12 mg/kg Single dose at 1 hour after surgery To evaluate the effect of PNU-282987 on behavioral outcomes and brain edema after intracerebral hemorrhage, results showed that PNU-282987 improved neurological function and reduced brain edema. PMC3293395
Mice Abdominal aortic aneurysm model in ApoE−/− mice Intraperitoneal injection 1 mg/kg Once daily for 4 weeks Activating α7nAChR slowed down AAA formation, reduced inflammatory responses, and inhibited NLRP3/caspase-1/GSDMD pathway-mediated cell pyroptosis. PMC9525652

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.32mL

0.66mL

0.33mL

16.60mL

3.32mL

1.66mL

33.20mL

6.64mL

3.32mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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