PNU282987 HCl
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MedKoo CAT#: 526847

CAS#: 123464-89-1 (HCl salt)

Description: PNU282987 is a drug that acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors. In animal studies, it shows nootropic effects, and derivatives may be useful in the treatment of schizophrenia, although PNU-282,987 is not suitable for use in humans because of excessive inhibition of the hERG antitarget.


Price and Availability

Size Price Shipping out time Quantity
10mg USD 90 2 Weeks
25mg USD 150 2 Weeks
50mg USD 250 2 Weeks
100mg USD 450 2 Weeks
200mg USD 650 2 Weeks
500mg USD 1250 2 Weeks
1g USD 2150 2 Weeks
2g USD 3850 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-27. Prices are subject to change without notice.

PNU282987 HCl purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 526847
Name: PNU282987 HCl
CAS#: 123464-89-1 (HCl salt)
Chemical Formula: C14H18Cl2N2O
Exact Mass:
Molecular Weight: 301.211
Elemental Analysis: C, 55.83; H, 6.02; Cl, 23.54; N, 9.30; O, 5.31


Synonym: PNU282987; PNU-282987; PNU 282987; PNU282,987; PNU-282,987; PNU 282,987; PNU282987 HCl; PNU282987 hydrochloride

IUPAC/Chemical Name: N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-4-chloro-benzamide monohydrochloride

InChi Key: HSEQUIRZHDYOIX-ZOWNYOTGSA-N

InChi Code: InChI=1S/C14H17ClN2O.ClH/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);1H/t13-;/m0./s1

SMILES Code: O=C(N[C@H]1CN2CCC1CC2)C3=CC=C(Cl)C=C3.[H]Cl


Technical Data

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


Additional Information

Related CAS#
CAS#123464-89-1 (PNU282987 HCl)
CAS#711085-63-1 (PNU282987 free base).


References

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2: Marcus MM, Björkholm C, Malmerfelt A, Möller A, Påhlsson N, Konradsson-Geuken Å, Feltmann K, Jardemark K, Schilström B, Svensson TH. Alpha7 nicotinic acetylcholine receptor agonists and PAMs as adjunctive treatment in schizophrenia. An experimental study. Eur Neuropsychopharmacol. 2016 Sep;26(9):1401-11. doi: 10.1016/j.euroneuro.2016.07.004. Epub 2016 Jul 26. PubMed PMID: 27474687.

3: Zhang Y, Cao SX, Sun P, He HY, Yang CH, Chen XJ, Shen CJ, Wang XD, Chen Z, Berg DK, Duan S, Li XM. Loss of MeCP2 in cholinergic neurons causes part of RTT-like phenotypes via α7 receptor in hippocampus. Cell Res. 2016 Jun;26(6):728-42. doi: 10.1038/cr.2016.48. Epub 2016 Apr 22. PubMed PMID: 27103432; PubMed Central PMCID: PMC4897179.

4: Fan BS, Zhang EH, Wu M, Guo JM, Su DF, Liu X, Yu JG. Activation of α7 Nicotinic Acetylcholine Receptor Decreases On-site Mortality in Crush Syndrome through Insulin Signaling-Na/K-ATPase Pathway. Front Pharmacol. 2016 Mar 29;7:79. doi: 10.3389/fphar.2016.00079. eCollection 2016. PubMed PMID: 27065867; PubMed Central PMCID: PMC4810156.

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6: Dong MW, Li M, Chen J, Fu TT, Lin KZ, Ye GH, Han JG, Feng XP, Li XB, Yu LS, Fan YY. Activation of α7nAChR Promotes Diabetic Wound Healing by Suppressing AGE-Induced TNF-α Production. Inflammation. 2016 Apr;39(2):687-99. doi: 10.1007/s10753-015-0295-x. PubMed PMID: 26650489.

7: Engel O, Akyüz L, da Costa Goncalves AC, Winek K, Dames C, Thielke M, Herold S, Böttcher C, Priller J, Volk HD, Dirnagl U, Meisel C, Meisel A. Cholinergic Pathway Suppresses Pulmonary Innate Immunity Facilitating Pneumonia After Stroke. Stroke. 2015 Nov;46(11):3232-40. doi: 10.1161/STROKEAHA.115.008989. Epub 2015 Oct 8. PubMed PMID: 26451017.

8: Navarro E, Buendia I, Parada E, León R, Jansen-Duerr P, Pircher H, Egea J, Lopez MG. Alpha7 nicotinic receptor activation protects against oxidative stress via heme-oxygenase I induction. Biochem Pharmacol. 2015 Oct 15;97(4):473-81. doi: 10.1016/j.bcp.2015.07.022. Epub 2015 Jul 23. PubMed PMID: 26212551.

9: Yang YH, Li DL, Bi XY, Sun L, Yu XJ, Fang HL, Miao Y, Zhao M, He X, Liu JJ, Zang WJ. Acetylcholine Inhibits LPS-Induced MMP-9 Production and Cell Migration via the α7 nAChR-JAK2/STAT3 Pathway in RAW264.7 Cells. Cell Physiol Biochem. 2015;36(5):2025-38. doi: 10.1159/000430170. Epub 2015 Jul 17. PubMed PMID: 26202362.

10: Lykhmus O, Gergalova G, Zouridakis M, Tzartos S, Komisarenko S, Skok M. Inflammation decreases the level of alpha7 nicotinic acetylcholine receptors in the brain mitochondria and makes them more susceptible to apoptosis induction. Int Immunopharmacol. 2015 Nov;29(1):148-51. doi: 10.1016/j.intimp.2015.04.007. Epub 2015 Apr 15. PubMed PMID: 25887272.

11: Tasaka Y, Yasunaga D, Kiyoi T, Tanaka M, Tanaka A, Suemaru K, Araki H. Involvement of stimulation of α7 nicotinic acetylcholine receptors in the suppressive effect of tropisetron on dextran sulfate sodium-induced colitis in mice. J Pharmacol Sci. 2015 Mar;127(3):275-83. doi: 10.1016/j.jphs.2014.12.016. Epub 2015 Feb 17. PubMed PMID: 25837923.

12: Kalashnyk O, Lykhmus O, Oliinyk O, Komisarenko S, Skok M. α7 Nicotinic acetylcholine receptor-specific antibody stimulates interleukin-6 production in human astrocytes through p38-dependent pathway. Int Immunopharmacol. 2014 Dec;23(2):475-9. doi: 10.1016/j.intimp.2014.09.022. Epub 2014 Oct 1. PubMed PMID: 25281899.

13: Leite PE, Gandía L, de Pascual R, Nanclares C, Colmena I, Santos WC, Lagrota-Candido J, Quirico-Santos T. Selective activation of α7 nicotinic acetylcholine receptor (nAChRα7) inhibits muscular degeneration in mdx dystrophic mice. Brain Res. 2014 Jul 21;1573:27-36. doi: 10.1016/j.brainres.2014.05.004. Epub 2014 May 14. PubMed PMID: 24833065.

14: Chen JK, Li ZP, Liu YZ, Zhao T, Zhao XB, Ni M, Jiang GJ, Shen FM. Activation of alpha 7 nicotinic acetylcholine receptor protects mice from radiation-induced intestinal injury and mortality. Radiat Res. 2014 Jun;181(6):666-71. doi: 10.1667/RR13575.1. Epub 2014 May 14. PubMed PMID: 24828112.

15: Kakinuma Y, Noguchi T, Okazaki K, Oikawa S, Iketani M, Kurabayashi A, Furihata M, Sato T. Antimuscle atrophy effect of nicotine targets muscle satellite cells partly through an α7 nicotinic receptor in a murine hindlimb ischemia model. Transl Res. 2014 Jul;164(1):32-45. doi: 10.1016/j.trsl.2014.02.005. Epub 2014 Apr 24. Erratum in: Transl Res. 2014 Dec;164(6):515. Kurabayashi, Mutsumi [corrected to Kurabayashi, Atsushi]. PubMed PMID: 24811002.

16: Shelukhina I, Paddenberg R, Kummer W, Tsetlin V. Functional expression and axonal transport of α7 nAChRs by peptidergic nociceptors of rat dorsal root ganglion. Brain Struct Funct. 2015 Jul;220(4):1885-99. doi: 10.1007/s00429-014-0762-4. Epub 2014 Apr 5. PubMed PMID: 24706047.

17: Narumoto O, Niikura Y, Ishii S, Morihara H, Okashiro S, Nakahari T, Nakano T, Matsumura H, Shimamoto C, Moriwaki Y, Misawa H, Yamashita N, Nagase T, Kawashima K, Yamashita N. Effect of secreted lymphocyte antigen-6/urokinase-type plasminogen activator receptor-related peptide-1 (SLURP-1) on airway epithelial cells. Biochem Biophys Res Commun. 2013 Aug 16;438(1):175-9. doi: 10.1016/j.bbrc.2013.07.048. Epub 2013 Jul 20. PubMed PMID: 23876317.

18: Parada E, Egea J, Buendia I, Negredo P, Cunha AC, Cardoso S, Soares MP, López MG. The microglial α7-acetylcholine nicotinic receptor is a key element in promoting neuroprotection by inducing heme oxygenase-1 via nuclear factor erythroid-2-related factor 2. Antioxid Redox Signal. 2013 Oct 10;19(11):1135-48. doi: 10.1089/ars.2012.4671. Epub 2013 Feb 25. PubMed PMID: 23311871; PubMed Central PMCID: PMC3785807.

19: Du MH, Hu Q, Luo HM, Lin ZL, Ma L, Wang H, Hu S. [Effects of PNU282987 on organ function and survival in dogs with lethal burn shock]. Zhongguo Wei Zhong Bing Ji Jiu Yi Xue. 2012 Nov;24(11):651-4. Chinese. PubMed PMID: 23131281.

20: Nirogi R, Kandikere V, Bhyrapuneni G, Saralaya R, Muddana N, Komarneni P. Methyllycaconitine: a non-radiolabeled ligand for mapping α7 neuronal nicotinic acetylcholine receptors - in vivo target localization and biodistribution in rat brain. J Pharmacol Toxicol Methods. 2012 Jul;66(1):22-8. doi: 10.1016/j.vascn.2012.05.003. Epub 2012 May 16. PubMed PMID: 22609758.