VU0357017 hydrochloride_product_DataBase

Bioactivity	VU0357017 hydrochloride (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1 muscarinic acetylcholine receptor, with an EC50 of 477 nM. VU0357017 hydrochloride is highly selective for M1 and has no activity at M2-M5 up to the highest concentrations tested (30 μM). VU0357017 hydrochloride can be used for the research of Alzheimer’s disease and schizophrenia[1][2][3].
Target	IC50: 477 nM (M1)
Invitro	VU0357017 is selective for M1 (Ki=9.91 µM) over M2-M5 mAChRs (Ki=21.4, 55.3, 35.0, and 50.0 μM, respectively) in CHO cells[1].VU0357017 (1 nM-100 μM) induces calcium release and ERK phosphorylation in a concentration-dependent manner in CHO cells[3].
In Vivo	VU0357017 (1-10 mg/kg, i.p.) reverses scopolamine-induced disruption of the contextual fear conditioning response[2]. Animal Model:
Name	VU0357017 hydrochloride
CAS	1135242-13-5
Formula	C18H28ClN3O3
Molar Mass	369.89
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[1]. Digby GJ, et al. Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode. ACS Chem Neurosci. 2012 Dec 19;3(12):1025-36. [2]. Lebois EP, et al. Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system. ACS Chem Neurosci. 2010;1(2):104-121. [3]. Digby GJ, et al. Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models. J Neurosci. 2012 Jun 20;32(25):8532-44.

PeptideDB

VU0357017 hydrochloride

CAS: 1135242-13-5 F: C18H28ClN3O3 W: 369.89