VU 0357017 hydrochloride

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Cat.No. 4295 - VU 0357017 hydrochloride | C18H27N3O3.HCl | CAS No. 1135242-13-5
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)
Datasheet
Citations (1)
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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
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Safety Datasheet

References

References are publications that support the products' biological activity.

Bridges et 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

Lebois et 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:


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Keywords: VU0357017 hydrochloride muscarinics acetylcholine machrs positive allosteric modulators pams m1 selective M1 Receptors

1 Citation for VU 0357017 hydrochloride

Citations are publications that use Tocris products. Selected citations for VU 0357017 hydrochloride include:

Jadeja et al (2016) Data regarding M1 muscarinic receptor-mediated modulation of hepatic catalase activity in response to oxidative stress. J Am Soc Nephrol 6 405 PMID: 26862589


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