LY 2033298
Tocris Bioscience, part of Bio-Techne | Catalog # 7027
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
Product Description
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).
Product Specifications
Molecular Weight
311.79
Formula
C13H14ClN3O2S
Storage
Store at +4°C
Purity
≥98% (HPLC)
Chemical Name
3-Amino-5-chloro-N-cyclopropyl-6-methoxy-4-methylthieno[2,3-b]pyridine-2-carboxamide
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
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 Specific Notices for LY 2033298
For research use only
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