CMPI hydrochloride

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Description: Potent positive allosteric modulator of α4β2 nAChRs; also inhibitor of (α4)2(β2)3, muscle-type and Torpedo nAChRs
Chemical Name: 3-(2-Chlorophenyl)-5-(5-methyl-1-(piperidin-4-yl)-1H-pyrazol-4-yl)isoxazole hydrochloride
Purity: ≥98% (HPLC)
Literature (2)

Biological Activity for CMPI hydrochloride

CMPI hydrochloride is a potent positive allosteric modulator of α4β2 nAChRs (EC50 values are 20 and 18 nM for rat and human, respectively). Selective for hα4β2 over hα3β2, hα3β4 and hα7. Inhibits (α4)2(β2)3, muscle-type and Torpedo nAChRs (IC50 values are 0.5, 0.7 and 0.2 μM, respectively), but not (α4)3(β2)2 receptors. Exhibits ability to photoincorporate into aliphatic and nucleophilic amino acid side chains.

Technical Data for CMPI hydrochloride

M. Wt 379.28
Formula C18H19ClN4O.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2250025-94-4
PubChem ID 127021040
Smiles CC1=C(C2=CC(C3=C(C=CC=C3)Cl)=NO2)C=NN1C4CCNCC4.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for CMPI hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
water 18.96 50
DMSO 37.93 100

Preparing Stock Solutions for CMPI hydrochloride

The following data is based on the product molecular weight 379.28. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.64 mL 13.18 mL 26.37 mL
5 mM 0.53 mL 2.64 mL 5.27 mL
10 mM 0.26 mL 1.32 mL 2.64 mL
50 mM 0.05 mL 0.26 mL 0.53 mL

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Product Datasheets for CMPI hydrochloride

References for CMPI hydrochloride

References are publications that support the biological activity of the product.

Hamouda (2016) Photolabeling a nicotinic acetylcholine receptor (nAChR) with an (α4)3(β2)2 nAChR-selective positive allosteric modulator. Mol.Pharmacol. 89 575 PMID: 26976945

Albrecht et al (2008) Discovery and optimization of substituted piperidines as potent, selective, CNS-penetrant α4β2 nicotinic acetylcholine receptor potentiators. Bioorg.Med.Chem.Lett. 18 5209 PMID: 18789861

Wang et al (2017) Unraveling amino acid residues critical for allosteric potentiation of (α4)3(β2)2-type nicotinic acetylcholine receptor responses. J.Biol.Chem. 292 9988 PMID: 28446611

If you know of a relevant reference for CMPI hydrochloride, please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Nicotinic ACh Receptors Scientific Review

Nicotinic ACh Receptors Scientific Review

Updated in 2014, this review by Sue Wonnacott summarizes the diverse structure and function of nicotinic acetylcholine receptors and gives an in-depth review of the ligands available for nAChR research. Compounds available from Tocris are listed.

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Alzheimer's disease (AD) is a debilitating and progressive neurodegenerative disease and the most common cause of dementia, affecting approximately 30% of individuals aged over 85 years. This poster summarizes the cellular and molecular mechanisms of AD.