| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C18H15FN4O |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
VU0453595 is a highly selective, systemically active positive allosteric modulator (PAM) of the M1 receptor, with an EC50 of 2140 nM, used in schizophrenia research[1][2]. It is supplied as an off-white to light yellow solid (C18H15FN4O, MW 322.34) at 99.44% purity.
Physical & Chemical Properties
| CAS Number | 1432436-13-9 |
|---|---|
| Molecular Formula | C18H15FN4O |
| Molecular Weight | 322.34 g/mol |
| Purity | 99.44% |
| Appearance | Solid |
| Color | Off-white to light yellow |
| SMILES | O=C1N(CC2=CC=C(C3=CN(C)N=C3)C=C2F)CC4=NC=CC=C41 |
| Target | mAChR1 |
| Signaling Pathway | GPCR/G Protein; Neuronal Signaling |
| Solubility | In Vitro: DMSO: 100 mg/mL (310.23 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (310.23 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (7.76 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (7.76 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Data provided by the manufacturer.
In Vitro
Treatment with M1 PAM VU0453595 (3 μM) leads to a transient rise in the excitability of medium spiny neurons (MSNs)[3].
In Vivo
VU0453595 enhances M1-mediated muscarinic long-term depression (mLTD)[1]. Behavioral deficits caused by repeated phencyclidine (PCP) administration are reversed by VU0453595 (1-10 mg/kg; i.p.)[1].
| Animal Model | Male C57BL6/J mice (8-9 weeks old)[1] |
|---|---|
| Dosage | 1, 3, or 10 mg/kg |
| Administration | Intraperitoneal (i.p.); 10 mL/kg; administered 30 min before the social interaction test |
| Result | Rescued deficits in social interaction observed in PCP-treated mice. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Nicotine and a positive allosteric modulator of m1 muscarinic receptor increase NMDA/AMPA ratio in the hippocampus and medial prefrontal cortex. Neuropharmacology 2025 Jan 1:262:110213. PMID: 39522675
Sex differences in interactions between the muscarinic-1 and orexin-1 receptors on cognitive flexibility in rats. Brain Res 2025 Nov 27:1872:150081. PMID: 41317779
