[CAS NO. 1135242-13-5] VU0357017hydrochloride
PRODUCTS SPECIFICATIONS [1135242-13-5]
DESCRIPTION [1135242-13-5]
Overview
| MDL | MFCD17215959 |
|---|---|
| Molecular Weight | 369.89 |
| Molecular Formula | C18H28ClN3O3 |
| SMILES | O=C(N1CCC(NCCNC(C2=CC=CC=C2C)=O)CC1)OCC.[H]Cl |
Summary
VU0357017 hydrochloride (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M 1 muscarinic acetylcholine receptor , with an EC 50 of 477 nM. VU0357017 hydrochloride is highly selective for M 1 and has no activity at M 2 -M 5 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] .
IC50 & Target
IC50: 477 nM (M1) [1]
In Vitro
VU0357017 is selective for M
1
(K
i
=9.91 µM) over M
2
-M
5
mAChRs (K
i
=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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
VU0357017 (1-10 mg/kg, i.p.) reverses scopolamine-induced disruption of the contextual fear conditioning response
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Sprague−Dawley rats (380-420 g) were pretreated with scopolamine [2] |
| Dosage: | 1, 3, 10 mg/kg |
| Administration: | A single i.p. |
| Result: | Produced a significant reversal of the scopolamine-induced deficits at a dose of 10 mg/kg. |
Appearance
Solid
Shipping
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)
Solvent & Solubility
H 2 O : 33.33 mg/mL ( 90.11 mM ; Need ultrasonic)
DMSO : 25 mg/mL ( 67.59 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.7035 mL | 13.5175 mL | 27.0351 mL |
| 5 mM | 0.5407 mL | 2.7035 mL | 5.4070 mL |
| 10 mM | 0.2704 mL | 1.3518 mL | 2.7035 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 33.33 mg/mL (90.11 mM); Clear solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.76 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.76 mM); Clear solution
References
- [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.