MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 526029 | Name: PNU-282987 free base
Featured New

Description:

WARNING: This product is for research use only, not for human or veterinary use.

PNU-282987 is a highly selective α7 nAChR agonist (Ki = 26 nM) displaying negligible blockade of α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM). PNU-282987 is inactive against a panel of 32 receptors at 1 μM, except 5-HT3 receptors (Ki = 930 nM).

Chemical Structure

PNU-282987 free base
PNU-282987 free base
CAS#711085-63-1 (free base)

Theoretical Analysis

MedKoo Cat#: 526029

Name: PNU-282987 free base

CAS#: 711085-63-1 (free base)

Chemical Formula: C14H17ClN2O

Exact Mass: 264.1029

Molecular Weight: 264.75

Elemental Analysis: C, 63.51; H, 6.47; Cl, 13.39; N, 10.58; O, 6.04

Price and Availability

Size Price Availability Quantity
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,350.00 2 Weeks
500mg USD 2,850.00 2 Weeks
1g USD 3,850.00 2 Weeks
2g USD 6,450.00 2 Weeks
Show More
Bulk Inquiry
Buy Now
Add to Cart
Related CAS #
711085-63-1 (free base) 123464-89-1 (HCl)
Synonym
PNU-282987; PNU 282987; PNU282987.
IUPAC/Chemical Name
Benzamide, N-(3R)-1-azabicyclo(2.2.2)oct-3-yl-4-chloro-
InChi Key
WECKJONDRAUFDD-ZDUSSCGKSA-N
InChi Code
InChI=1S/C14H17ClN2O/c15-12-3-1-11(2-4-12)14(18)16-13-9-17-7-5-10(13)6-8-17/h1-4,10,13H,5-9H2,(H,16,18)/t13-/m0/s1
SMILES Code
O=C(N[C@H]1CN2CCC1CC2)C3=CC=C(Cl)C=C3
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PNU-282987 is a highly selective α7 nAChR agonist (Ki = 26 nM).
In vitro activity:
In the present study, using pharmacological inhibition and genetic knockout of α7nAChR, this study assessed the antiapoptotic effects of an α7nAChR agonist PNU-282987 in primary cultured astrocytes treated with 1-methyl-4-phenylpyridinium (MPP+). PNU-282987 promoted the viability of astrocytes, alleviated MPP+ induced apoptosis, and decreased the number of GFAP+/TUNEL+ cells. Meanwhile, PNU-282987 upregulated the expression of the antiapoptotic protein Bcl-2 and downregulated the expression of the apoptotic protein Bax and cleaved-caspase-3. Moreover, the suppression of the JNK-p53-caspase-3 signaling may underlie the neuroprotective property of PNU-282987. Therefore, PNU-282987 ameliorates astroglial apoptosis induced by MPP+ through α7nAChR-JNK-p53 signaling. Reference: Front Cell Neurosci. 2019 Nov 12;13:507. https://pubmed.ncbi.nlm.nih.gov/31780901/
In vivo activity:
Amphetamine-induced sensory gating deficit, determined by auditory-evoked potentials in hippocampal CA3 region, was restored by systemic administration of PNU-282987 in chloral hydrate-anesthetized rats. Auditory gating of rat reticular thalamic neurons was also disrupted by amphetamine; however, PNU-282987 normalized gating deficit only in a subset of tested neurons (6 of 11). Furthermore, PNU-282987 improved the inherent hippocampal gating deficit occurring in a subpopulation of anesthetized rats, and enhanced amphetamine-induced hippocampal oscillation. This study proposes that the alpha7 nAChR agonist PNU-282987, via modulating/enhancing hippocampal GABAergic neurotransmission, improves auditory gating and enhances hippocampal oscillatory activity. Reference: J Pharmacol Exp Ther. 2005 Mar;312(3):1213-22. https://pubmed.ncbi.nlm.nih.gov/15523001/
Solvent mg/mL mM comments
Solubility
PBS (pH 7.2) 5.0 18.89
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 264.75 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Zhang Y, Ma R, Wang W, Deng Q, Cao C, Yu C, Li S, Shi L, Tian J. Activation of α7nAChR by PNU282987 improves cognitive impairment through inhibiting oxidative stress and neuroinflammation in D-galactose induced aging via regulating α7nAChR/Nrf2/HO-1 signaling pathway. Exp Gerontol. 2023 May;175:112139. doi: 10.1016/j.exger.2023.112139. Epub 2023 Mar 10. PMID: 36898594. 2. Hua Y, Yang B, Chen Q, Zhang J, Hu J, Fan Y. Activation of α7 Nicotinic Acetylcholine Receptor Protects Against 1-Methyl-4-Phenylpyridinium-Induced Astroglial Apoptosis. Front Cell Neurosci. 2019 Nov 12;13:507. doi: 10.3389/fncel.2019.00507. PMID: 31780901; PMCID: PMC6861188. 3. Spitsbergen JB, Webster SE, Linn CL. Functional Changes in the Adult Mouse Retina using an Alpha7 Nicotinic Acetylcholine Receptor Agonist after Blast Exposure. Neuroscience. 2023 Feb 21;512:1-15. doi: 10.1016/j.neuroscience.2022.12.017. Epub 2022 Dec 24. PMID: 36572172. 4. Hajós M, Hurst RS, Hoffmann WE, Krause M, Wall TM, Higdon NR, Groppi VE. The selective alpha7 nicotinic acetylcholine receptor agonist PNU-282987 [N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-4-chlorobenzamide hydrochloride] enhances GABAergic synaptic activity in brain slices and restores auditory gating deficits in anesthetized rats. J Pharmacol Exp Ther. 2005 Mar;312(3):1213-22. doi: 10.1124/jpet.104.076968. Epub 2004 Nov 2. PMID: 15523001.
In vitro protocol:
1. Zhang Y, Ma R, Wang W, Deng Q, Cao C, Yu C, Li S, Shi L, Tian J. Activation of α7nAChR by PNU282987 improves cognitive impairment through inhibiting oxidative stress and neuroinflammation in D-galactose induced aging via regulating α7nAChR/Nrf2/HO-1 signaling pathway. Exp Gerontol. 2023 May;175:112139. doi: 10.1016/j.exger.2023.112139. Epub 2023 Mar 10. PMID: 36898594. 2. Hua Y, Yang B, Chen Q, Zhang J, Hu J, Fan Y. Activation of α7 Nicotinic Acetylcholine Receptor Protects Against 1-Methyl-4-Phenylpyridinium-Induced Astroglial Apoptosis. Front Cell Neurosci. 2019 Nov 12;13:507. doi: 10.3389/fncel.2019.00507. PMID: 31780901; PMCID: PMC6861188.
In vivo protocol:
1. Spitsbergen JB, Webster SE, Linn CL. Functional Changes in the Adult Mouse Retina using an Alpha7 Nicotinic Acetylcholine Receptor Agonist after Blast Exposure. Neuroscience. 2023 Feb 21;512:1-15. doi: 10.1016/j.neuroscience.2022.12.017. Epub 2022 Dec 24. PMID: 36572172. 2. Hajós M, Hurst RS, Hoffmann WE, Krause M, Wall TM, Higdon NR, Groppi VE. The selective alpha7 nicotinic acetylcholine receptor agonist PNU-282987 [N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-4-chlorobenzamide hydrochloride] enhances GABAergic synaptic activity in brain slices and restores auditory gating deficits in anesthetized rats. J Pharmacol Exp Ther. 2005 Mar;312(3):1213-22. doi: 10.1124/jpet.104.076968. Epub 2004 Nov 2. PMID: 15523001.
1: Xu FF, Li ZC, Zhang WJ, Li Q, Li DJ, Meng HB, Shen FM, Fu H. Activation of α7 nicotinic acetylcholine receptors inhibits hepatic necroptosis and ameliorates acute liver injury in mice. Anesthesiology. 2024 Aug 26. doi: 10.1097/ALN.0000000000005206. Epub ahead of print. PMID: 39186677. 2: AlSharari SD, Alameen AA, Aldafiri FS, Ali YS, Alshammari MA, Sari Y, Damaj MI. Activation of α7 nicotinic receptors attenuated hyperalgesia and anxiety induced by palatable obesogenic diet withdrawal. J Pharmacol Sci. 2024 Oct;156(2):86-101. doi: 10.1016/j.jphs.2024.07.006. Epub 2024 Jul 22. PMID: 39179339. 3: Lykhmus O, Tzeng WY, Koval L, Uspenska K, Zirdum E, Kalashnyk O, Garaschuk O, Skok M. Impairment of brain function in a mouse model of Alzheimer's disease during the pre-depositing phase: The role of α7 nicotinic acetylcholine receptors. Biomed Pharmacother. 2024 Sep;178:117255. doi: 10.1016/j.biopha.2024.117255. Epub 2024 Aug 7. PMID: 39116785. 4: Alameen AA, AlSharari SD, Alshammari MA, Damaj MI, Sari Y. The potential effect of α7 nicotinic receptors modulation on palatable food-induced dependence-like behaviors. Saudi Pharm J. 2024 Aug;32(8):102138. doi: 10.1016/j.jsps.2024.102138. Epub 2024 Jul 4. PMID: 39109164; PMCID: PMC11301368. 5: Chen F, Zhang Z, Zhang H, Guo P, Feng J, Shen H, Liu X. Activation of α7 Nicotinic Acetylcholine Receptor Improves Muscle Endurance by Upregulating Orosomucoid Expression and Glycogen Content in Mice. J Cell Biochem. 2024 Jul 16:e30630. doi: 10.1002/jcb.30630. Epub ahead of print. PMID: 39014907. 6: Vanzo-Sparks HK, Webster SE, Webster MK, Linn CL. Quantification of Proliferating and Mitotically Active Retinal Cells in Mice by Flow Cytometry. Bio Protoc. 2024 Jul 5;14(13):e5024. doi: 10.21769/BioProtoc.5024. PMID: 39011369; PMCID: PMC11247376. 7: Shen L, Zhong X, Ji H, Yang S, Jin J, Lyu C, Ren Y, Xiao Y, Zhang Y, Fang S, Lin N, Tou J, Shu Q, Lai D. Macrophage α7nAChR alleviates the inflammation of neonatal necrotizing enterocolitis through mTOR/NLRP3/IL-1β pathway. Int Immunopharmacol. 2024 Sep 30;139:112590. doi: 10.1016/j.intimp.2024.112590. Epub 2024 Jul 13. PMID: 38996778. 8: Linn DM. Target identification and validation of the alpha7 nicotinic acetylcholine receptor as a potential therapeutic target in retinal disease. Front Ophthalmol (Lausanne). 2023 Jul 24;3:1190439. doi: 10.3389/fopht.2023.1190439. PMID: 38983049; PMCID: PMC11182235. 9: Wu L, Li J, Zou J, Tang D, Chen R. Vagus nerve modulates acute-on-chronic liver failure progression via CXCL9. Chin Med J (Engl). 2024 Jun 28. doi: 10.1097/CM9.0000000000003104. Epub ahead of print. PMID: 38945689. 10: Chen SH, Damborsky JC, Wilson BC, Fannin RD, Ward JM, Gerrish KE, He B, Martin NP, Yakel JL. α7 nicotinic receptor activation mitigates herpes simplex virus type 1 infection in microglia cells. Antiviral Res. 2024 Aug;228:105934. doi: 10.1016/j.antiviral.2024.105934. Epub 2024 Jun 15. PMID: 38880195; PMCID: PMC11250235. 11: Ongnok B, Prathumsap N, Chunchai T, Pantiya P, Arunsak B, Chattipakorn N, Chattipakorn SC. Nicotinic and Muscarinic Acetylcholine Receptor Agonists Counteract Cognitive Impairment in a Rat Model of Doxorubicin-Induced Chemobrain via Attenuation of Multiple Programmed Cell Death Pathways. Mol Neurobiol. 2024 Apr 3. doi: 10.1007/s12035-024-04145-0. Epub ahead of print. PMID: 38568417. 12: Xia XM, Duan Y, Wang YP, Han RX, Dong YF, Jiang SY, Zheng Y, Qiao C, Cao L, Lu X, Lu M. Vagus nerve stimulation as a promising neuroprotection for ischemic stroke via α7nAchR-dependent inactivation of microglial NLRP3 inflammasome. Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365. doi: 10.1038/s41401-024-01245-4. Epub 2024 Mar 19. PMID: 38504011; PMCID: PMC11192746. 13: Zhang X, Wang H, Cai X, Zhang A, Liu E, Li Z, Jiang T, Li D, Ding W. α7nAChR Activation Combined with Endothelial Progenitor Cell Transplantation Attenuates Lung Injury in Diabetic Rats with Sepsis through the NF-κB Pathway. Inflammation. 2024 Aug;47(4):1344-1355. doi: 10.1007/s10753-024-01980-0. Epub 2024 Feb 1. PMID: 38302679. 14: Tsotsokou G, Kouri V, Papatheodoropoulos C. α7 nicotinic acetylcholine receptors induce long-term synaptic enhancement in the dorsal but not ventral hippocampus. Synapse. 2024 Jan;78(1):e22285. doi: 10.1002/syn.22285. PMID: 38287475. 15: Takizawa S, Ohuchi K, Fujimaki A, Ito T, Murakami T, Kurita H, Inden M. Effects of α7 nicotinic acetylcholine receptor agonist against α-synuclein- induced neurotoxicity. Neurosci Lett. 2024 Feb 16;823:137654. doi: 10.1016/j.neulet.2024.137654. Epub 2024 Jan 26. PMID: 38281695. 16: Banzato R, Pinheiro-Menegasso NM, Novelli FPRS, Olivo CR, Taguchi L, de Oliveira Santos S, Fukuzaki S, Teodoro WPR, Lopes FDTQS, Tibério IFLC, de Toledo-Arruda AC, Prado MAM, Prado VF, Prado CM. Alpha-7 Nicotinic Receptor Agonist Protects Mice Against Pulmonary Emphysema Induced by Elastase. Inflammation. 2024 Jun;47(3):958-974. doi: 10.1007/s10753-023-01953-9. Epub 2024 Jan 16. PMID: 38227123. 17: Li WW, Shi XY, Wei T, Guo TZ, Kingery WS, Clark JD. Alpha-7 Nicotinic Acetylcholine Receptor Activation Inhibits Trauma Induced Pronociceptive Autoimmune Responses. J Pain. 2024 May;25(5):104422. doi: 10.1016/j.jpain.2023.11.005. Epub 2023 Nov 10. PMID: 37951284; PMCID: PMC11058031. 18: Fu S, Ni T, Zhang M, Ren D, Feng Y, Yao N, Zhang X, Wang R, Xu W, Yang N, Yang Y, He Y, Zhao Y, Liu J. Cholinergic Anti-inflammatory Pathway Attenuates Acute Liver Failure Through Inhibiting MAdCAM1/α4β7-mediated Gut-derived Proinflammatory Lymphocytes Accumulation. Cell Mol Gastroenterol Hepatol. 2024;17(2):199-217. doi: 10.1016/j.jcmgh.2023.10.012. Epub 2023 Nov 4. PMID: 37926366; PMCID: PMC10758884. 19: Prathumsap N, Ongnok B, Khuanjing T, Arinno A, Maneechote C, Chunchai T, Arunsak B, Kerdphoo S, Chattipakorn SC, Chattipakorn N. Acetylcholine receptor agonists effectively attenuated multiple program cell death pathways and improved left ventricular function in trastuzumab-induced cardiotoxicity in rats. Life Sci. 2023 Sep 15;329:121971. doi: 10.1016/j.lfs.2023.121971. Epub 2023 Jul 22. PMID: 37482212. 20: Xie Y, Tao S, Pan B, Yang W, Shao W, Fang X, Han D, Li J, Zhang Y, Chen R, Li W, Xu Y, Kan H. Cholinergic anti-inflammatory pathway mediates diesel exhaust PM2.5-induced pulmonary and systemic inflammation. J Hazard Mater. 2023 Sep 15;458:131951. doi: 10.1016/j.jhazmat.2023.131951. Epub 2023 Jun 27. PMID: 37392642.