LY 2033298

Key Product Details

Product Description

LY 2033298 is a selective positive allosteric modulator of M₄ receptor (K_B = 200 nM, α = 35); increases the potency of acetylcholine by 40-fold. Exhibits no effect at hM_1/3/5 receptors and a small effect at hM₂ (K_B = 1 μM α = 3.7). Potentiates other full and partial orthosteric agonists, including Carbachol, Oxotremorine-M, and McN-A343. Does not affect binding of antagonist NMS. Active in vivo. Antipsychotic.

α indicates the degree of allosteric enhancement when both orthosteric and allosteric sites are occupied (derived from the allosteric ternary complex model).

Product Specifications for LY 2033298

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for LY 2033298

The following data is based on the product molecular weight 311.79.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

1 Recalculate

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.21 mL	16.04 mL	32.07 mL
5 mM	0.64 mL	3.21 mL	6.41 mL
10 mM	0.32 mL	1.60 mL	3.21 mL
50 mM	0.06 mL	0.32 mL	0.64 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Huynh Synthesis and pharmacological evaluation of M₄ muscarinic receptor positive allosteric modulators derived from VU10004. ACS Chem. Neurosci. 2015 PMID: 25857219
• Chan Allosteric modulation of the muscarinic M₄ receptor as an approach to treating schizophrenia Proc.Natl.Acad.Sci.U.S.A. 2008 PMID: 18678919
• Leach Molecular mechanisms of action and in vivo validation of an M₄ muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties. Neuropsychopharmacology 2010 PMID: 19940843

Product Documents for LY 2033298