Description: Positive allosteric modulator of M1 receptors
Chemical Name: 4-[[2-[(2-Methylbenzoyl)amino]ethyl]amino]-1-piperidinecarboxylic acid ethyl ester hydrochloride
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Positive allosteric modulator of muscarinic M1 receptors (EC50 = 198 nM). Displays no activity at M2-M5 at concentrations up to 30 μM. Potentiates NMDA receptor currents in hippocampal neurons; activity reverses cognitive decifits in a rodent model of hippocampal-dependent memory. CNS penetrant.
Technical Data
M. Wt
369.89
Formula
C18H27N3O3.HCl
Storage
Store at +4°C
Purity
≥98% (HPLC)
CAS Number
1135242-13-5
PubChem ID
25010775
InChI Key
XKJQVUIXSBOCPP-UHFFFAOYSA-N
Smiles
CC1=CC=CC=C1C(NCCNC2CCN(C(OCC)=O)CC2)=O.Cl
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
1.85
5
water
9.25
25
Preparing Stock Solutions
The following data is based on the product molecular weight 369.89. 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
2.7 mL
13.52 mL
27.04 mL
5 mM
0.54 mL
2.7 mL
5.41 mL
10 mM
0.27 mL
1.35 mL
2.7 mL
50 mM
0.05 mL
0.27 mL
0.54 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Bridgeset al (2010) Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) Lead. Part II. Development of potent and highly selective M1 PAM. Bioorg.Med.Chem.Lett. 20 1972 PMID: 20156687
Leboiset al (2010) Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M1 receptor function in the central nervous system. ACS Chem.Neurosci. 1 104 PMID: