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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
|Storage||Store at -20°C|
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|
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.
|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|
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
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Keywords: CMPI hydrochloride, CMPI hydrochloride supplier, PAM, positive, allosteric, modulator, Inhibitors, inhibits, CMPI, nAChR, nAChRs, a4b2, alpha4beta2, α4β2, nicotinic, acetylcholine, receptors, photoreactive, Nicotinic, (a4b2), Receptors, (Other, Subtypes), 5963, Tocris Bioscience
Citations for CMPI hydrochloride
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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!
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Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.