PNU-282987
Based on 15 publication(s) in Google Scholar
PNU-282987 is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 can be used for the research of central and peripheral nervous systems.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.93%
- CAS. Nr.: 123464-89-1
- Formel: C14H18Cl2N2O
- Molecular Weight:301.21
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) PNU-282987
More- Int J Biol Macromol. 2026 Mar:349:150933. [Abstract]
- Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365. [Abstract]
- Free Radic Biol Med. 2025 Apr 3:S0891-5849(25)00207-2. [Abstract]
- Cell Death Discov. 2022 Mar 30;8(1):141. [Abstract]
- Mol Med. 2022 Sep 4;28(1):104. [Abstract]
- Biochem Pharmacol. 2025 Aug 29;242(Pt 1):117290. [Abstract]
- Inflamm Res. 2023 Apr;72(4):879-892. [Abstract]
- Respir Res. 2026 Apr 1;27(1):206. [Abstract]
- Int Immunopharmacol. 2025 Jan 1:147:113941. [Abstract]
- Eur J Pharmacol. 2021 Jun 5:900:174067. [Abstract]
- Cell Signal. 2024 Jun 26:111275. [Abstract]
- J Cell Biochem. 2024 Jul 16:e30630. [Abstract]
- J Pain Res. 2021 Feb 15:14:441-452. [Abstract]
- Biomed Res. 2017; Special Issue: ISSN 0970.
- Biomed Res-India. 2019 Apr.
Customer Validation & Images
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Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
IC50: 4541nM (5-HT3); EC50: 154 nM (α7 nAChR); Ki: 27 nM (R7 MLA)[1]
PNU-282987 (Compound C7) displaces the R7 selective antagonist methyllycaconitine (MLA) from rat brain homogenates with a Ki of 27 nM[1].
PNU-282987 has α7 nAChR agonist activity with an EC50 of 154 nM[1].
PNU-282987 also has inhibition for the 5-HT3 receptor with an IC50 value of 4541nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PNU-282987 (30 μM) evokes currents in rat hippocampal neurons in a concentration-dependent and MLA blockable manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[1]
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Dosage:1, 3 mg/kg
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Administration:i.v.
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Result:Significantly reversed amphetamine-induced gating deficit.
Chemical Information
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CAS. Nr. 123464-89-1
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Appearance Solid
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Molecular Weight 301.21
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Formel C14H18Cl2N2O
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Color White to off-white
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SMILES
O=C(C1=CC=C(C=C1)Cl)N[C@H]2CN3CCC2CC3.[H]Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (15)
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Journal Impact Factor
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Most Recent
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Int J Biol Macromol
α-Conotoxin LvID, an antagonist of α7 nicotinic acetylcholine receptor, mitigates Alzheimer-associated phenotypes by inhibiting Aβ deposition and reactive astrogliosis. [Abstract]2026 Mar:349:150933. PMID: 41692211 -
Acta Pharmacol Sin
Vagus nerve stimulation as a promising neuroprotection for ischemic stroke via α7nAchR-dependent inactivation of microglial NLRP3 inflammasome. [Abstract]2024 Jul;45(7):1349-1365. PMID: 38504011
PNU-282987 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365. [Abstract]
PNU-282987 (0.1 μM; 1 h) reduced Nlrp3 mRNA level in the oxygen-glucose deprivation/reperfusion (OGD/R) model performed in BV2 cells.
PNU-282987 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365. [Abstract]
PNU-282987 (0.1 μM; 1 h) diminished the upregulation of NLRP3 expression induced by LPS + ATP in BV2 cells.
PNU-282987 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365. [Abstract]
PNU-282987 (0.1 μM; 1 h) blocked conspicuous nucleus translocation by LPS + ATP stimulation in BV2 cells.
PNU-282987 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365. [Abstract]
PNU-282987 (0.1 μM; 1 h) reduced the release of IL-1β in the conditioned medium collected from BV2 cells.
PNU-282987 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365. [Abstract]
PNU-282987 (0.1 μM; 1 h) significantly ameliorated the apoptosis of PC12 cells induced by the LPS + ATP-containing conditioned medium.
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Free Radic Biol Med
Ultrasound-responsive taurine lipid nanoparticles attenuate oxidative stress and promote macrophage polarization for diabetic wound healing. [Abstract]2025 Apr 3:S0891-5849(25)00207-2. PMID: 40187503 -
Cell Death Discov
Alpha-7 nicotinic acetylcholine receptor agonist alleviates psoriasis-like inflammation through inhibition of the STAT3 and NF-κB signaling pathway. [Abstract]2022 Mar 30;8(1):141. PMID: 35351863 -
Mol Med
Protective effect of α7 nicotinic acetylcholine receptor activation on experimental colitis and its mechanism. [Abstract]2022 Sep 4;28(1):104. PMID: 36058917 -
Biochem Pharmacol
α7nAChR activation promotes the generation of Treg cells by enhancing the dephosphorylation of Foxo1 via the IP3R/Ca2+/calcineurin pathway. [Abstract]2025 Aug 29;242(Pt 1):117290. PMID: 40886855 -
Inflamm Res
Activating α7nAChR helps post-myocardial infarction healing by regulating macrophage polarization via the STAT3 signaling pathway. [Abstract]2023 Apr;72(4):879-892. PMID: 36912917
PNU-282987 purchased from MedChemExpress. Usage Cited in: Inflamm Res. 2023 Apr;72(4):879-892. [Abstract]
PNU-282987 (3 mg/kg; i.p.; single daily for consecutively 28 days) signifcantly decreases the expression levels of collagen I, collagen III, and α-SMA in myocardial infarction (MI) rats model, while Methyllycaconitine citrate (MLA; 3 mg/kg; i.p.; single daily for consecutively 28 days) increases these proteins levels.
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Respir Res
Activation of α7nAChR prevents maladaptive right ventricular remodeling via inhibiting the recruitment of CCR2+ macrophages in experimental pulmonary arterial hypertension. [Abstract]2026 Apr 1;27(1):206. PMID: 41923075 -
Int Immunopharmacol
Electroacupuncture promotes resolution of inflammation by modulating SPMs via vagus nerve activation in LPS-induced ALI. [Abstract]2025 Jan 1:147:113941. PMID: 39746272 -
Eur J Pharmacol
Activation of alpha7 nicotinic acetylcholine receptor protects bovine endometrial tissue against LPS-induced inflammatory injury via JAK2/STAT3 pathway and COX-2 derived prostaglandin E2. [Abstract]2021 Jun 5:900:174067. PMID: 33811838 -
Cell Signal
2024 Jun 26:111275. PMID: 38942343 -
J Cell Biochem
Activation of α7 Nicotinic Acetylcholine Receptor Improves Muscle Endurance by Upregulating Orosomucoid Expression and Glycogen Content in Mice. [Abstract]2024 Jul 16:e30630. PMID: 39014907 -
J Pain Res
The Spinal α7-Nicotinic Acetylcholine Receptor Contributes to the Maintenance of Cancer-Induced Bone Pain. [Abstract]2021 Feb 15:14:441-452. PMID: 33623426 -
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Lösungsmittel & Löslichkeit
H2O : 50 mg/mL (166.00 mM; Need ultrasonic)
DMSO : 17.5 mg/mL (58.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 1 mg/mL (3.32 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (166.00 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO / H2O | 1 mM | 3.3199 mL | 16.5997 mL | 33.1994 mL | 82.9986 mL |
| 5 mM | 0.6640 mL | 3.3199 mL | 6.6399 mL | 16.5997 mL | |
| 10 mM | 0.3320 mL | 1.6600 mL | 3.3199 mL | 8.2999 mL | |
| 15 mM | 0.2213 mL | 1.1066 mL | 2.2133 mL | 5.5332 mL | |
| 20 mM | 0.1660 mL | 0.8300 mL | 1.6600 mL | 4.1499 mL | |
| 25 mM | 0.1328 mL | 0.6640 mL | 1.3280 mL | 3.3199 mL | |
| 30 mM | 0.1107 mL | 0.5533 mL | 1.1066 mL | 2.7666 mL | |
| 40 mM | 0.0830 mL | 0.4150 mL | 0.8300 mL | 2.0750 mL | |
| 50 mM | 0.0664 mL | 0.3320 mL | 0.6640 mL | 1.6600 mL | |
| H2O | 60 mM | 0.0553 mL | 0.2767 mL | 0.5533 mL | 1.3833 mL |
| 80 mM | 0.0415 mL | 0.2075 mL | 0.4150 mL | 1.0375 mL | |
| 100 mM | 0.0332 mL | 0.1660 mL | 0.3320 mL | 0.8300 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
PNU-282987 Related Classifications
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