LY 2033298

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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)
Literature (1)

Biological Activity for LY 2033298

LY 2033298 is a selective positive allosteric modulator of M4 receptor (KB = 200 nM, α = 35); increases the potency of acetylcholine by 40-fold. Exhibits no effect at hM1/3/5 receptors and a small effect at hM2 (KB = 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

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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
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 Data for LY 2033298

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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 1.6 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.

Leach et al (2010) Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties. Neuropsychopharmacology 35 855 PMID: 19940843

Huynh et al (2015) Synthesis and pharmacological evaluation of M4 muscarinic receptor positive allosteric modulators derived from VU10004. ACS Chem. Neurosci. 6 838 PMID: 25857219

Chan et al (2008) Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophrenia Proc.Natl.Acad.Sci.U.S.A. 105 10978 PMID: 18678919

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Citations for LY 2033298

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