CMPI hydrochloride

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Cat.No. 5963 - CMPI hydrochloride | C18H19ClN4O.HCl
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

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

M. Wt 379.28
Formula C18H19ClN4O.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
PubChem ID 127021040
InChI Key WNKFVIPYZXTQBR-UHFFFAOYSA-N
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

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

Preparing Stock Solutions

The following data is based on the product molecular weight 379.28. Batch specific molecular weights may vary from batch to batch due to solvent 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

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References

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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Literature in this Area

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