LY 2033298

Catalog # Availability Size / Price Qty
7027/25
7027/5
LY 2033298 | CAS No. 886047-13-8 | mAChR M4 Modulators
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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

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Biological Activity

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).

Technical Data

Formula:
C13H14ClN3O2S
Solubility:
Soluble to 100 mM in DMSO and to 20 mM in ethanol
Storage:
Store the unopened product at 2 - 8 °C. Do not use past expiration date.
CAS No:
886047-13-8

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.

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