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VU0357017 hydrochloride

Cat. No. M5194

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VU0357017 hydrochloride Structure
Synonym:

VU0357017 HCl

Size Price Availability Quantity
5mg USD 87  USD87 In stock
10mg USD 149  USD149 In stock
50mg USD 549  USD549 In stock
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Quality Control & Documentation
Biological Activity

VU0357017 hydrochloride is a highly selective M1 agonist. VU0357017 hydrochloride acts at an allosteric site to activate the receptor. Ki values of VU0357017 derived from competition binding experiment is 9.91(rM1), 21.4 (rM2), 55.3 (rM3), 35 (rM4), and 50 (rM5), respectively. VU0357017 has robust effects on M1-activation of calcium mobilization and ERK1/2 phosphorylation but have little effect on β-arrestin recruitment. VU0357017 HCl induces calcium release and ERK phosphorylation but is without effects on β-arrestin recruitment. VU0357017 HCl enhances performance in Morris water maze and contextual fear conditioning in rats.

Chemical Information
Molecular Weight 369.89
Formula C18H28ClN3O3
CAS Number 1135242-13-5
Solubility (25°C) DMSO 24 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Digby GJ, et al. ACS Chem Neurosci. Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode.

[2] Digby GJ, et al. J Neurosci. Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models.

[3] Lebois EP, et al. ACS Chem Neurosci. Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system.

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