LY 2033298

Name: LY 2033298
Brand: Tocris Bioscience
SKU: 7027

Tocris Bioscience, part of Bio-Techne | Catalog # 7027

COA / SDS

Selective positive allosteric modulator of M4 receptors; active in vivo; antipsychotic

Key Product Details

Description:	Selective positive allosteric modulator of M₄ receptors; active in vivo; antipsychotic
Chemical Name:	3-Amino-5-chloro-N-cyclopropyl-6-methoxy-4-methylthieno[2,3-b]pyridine-2-carboxamide
Purity:	≥98% (HPLC)
Molecular Weight:	311.79

View Full Technical Details for LY 2033298

Technical Data
Citations

Biological Activity for LY 2033298

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).

Compound Libraries for LY 2033298

LY 2033298 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for LY 2033298

M. Wt	311.79
Formula	C₁₃H₁₄ClN₃O₂S
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	886047-13-8
PubChem ID	11536903
InChi Key	CTEGQKDJTBWFHW-UHFFFAOYSA-N
Smiles	NC1=C(C(NC2CC2)=O)SC3=NC(OC)=C(Cl)C(C)=C31

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for LY 2033298

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	31.18	100
	ethanol	6.24	20

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for LY 2033298

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