VU0152100

SKU: orb1307615

Description

VU0152100 is a selective allosteric potentiator of the muscarinic acetylcholine receptor M4, exhibiting an EC50 of 380 nM. This compound is a valuable research tool for investigating M4 receptor function in both in vitro assays and in vivo models related to neuroscience and CNS disorders.

Research Area

Neuroscience

Key Properties

• CAS Number: 409351-28-6
• MW: 341.43
• Purity: 99.56% (May vary between batches)
• Formula: C₁₈H₁₉N₃O₂S
• SMILES: COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)cc1
• Target: AChR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.86 mM);DMSO:55 mg/mL (161.09 mM)

Bioactivity

• In Vivo:
  Systemic administration of VU0152099 and VU0152100 provides robust brain levels of these compounds, the effects of VU0152099 and VU0152100 were evaluated in reversing amphetamine-induced hyperlocomotion in rats using a dose of 56.6 mg/kg i.p. for each compound with a 30-min pretreatment interval .
• In Vitro:
  VU0152100 was selective for M4 relative to M1, M2, M3, and M5. VU0152100 dose-dependently potentiated the response to an EC20 concentration of ACh (EC50: 1.9 ± 0.2 μM) and increased the maximal response to ACh to approximately 130%. VU0152100 (10 μM) also increased the potency of ACh to induce GIRK-mediated thallium flux, as manifest by a robust (≈30-fold) leftward shift in the ACh CRC from 77 ± 1.2 nM (veh) to 2.35 ± 0.5 nM .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Muscarinic acetylcholine receptor, inhibit, mAChR, M4 mAChR, Inhibitor, VU152100, VU-152100, VU 0152100, VU 152100, VU0152100, VU-0152100

Compound Identifiers

PubChem CID

864492

Paulina Cieślik 1, Anna Rafało-Ulińska 1, Joanna M Wierońska Prevention of MK-801-induced amnestic effect with combined activation of 5-HT1A and muscarinic receptors in mice Pharmacol Biochem Behav, (2024)

PubMed: 38462045