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Xanomeline oxalate

Chemical Structure : Xanomeline oxalate

CAS No.: 141064-23-5

Xanomeline oxalate (LY246708;LY-246708;NNC 110232)

Catalog No.: PC-43517Not For Human Use, Lab Use Only.

Xanomeline oxalate (LY246708, NNC 110232) is a potent, specific M1 muscarinic agonist with functional selectivity for M1 receptor (binding IC50 of 6 pM in the rabbit vas deferens).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Xanomeline oxalate (LY246708, NNC 110232) is a potent, specific M1 muscarinic agonist with functional selectivity for M1 receptor (binding IC50 of 6 pM in the rabbit vas deferens); displays low affinity for M2 receptors in guinea pig atria (EC50=3 uM); xanomeline increases striatal levels of dopamine metabolites, presumably by acting at M1 heteroreceptors on dopamine neurons to increase dopamine release in vivo; inhibits ex vivo binding of muscarinic radioligands to homogenates of brain and the inhibition of ex vivo binding occurred in the same dose range as increases in DOPAC levels; xanomeline is selective agonist for M1 over M2 and M3 receptors in vivo in rats.

Alzheimer Disease

Phase 3 Discontinued

Physicochemical Properties

M.Wt
Formula C16H25N3O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Pyridine, 3-[4-(hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methyl-, ethanedioate (1:1)

References

1. Shannon HE, et al. J Pharmacol Exp Ther. 1994 Apr;269(1):271-81.

2. Sauerberg P, et al. J Med Chem. 1992 Jun 12;35(12):2274-83.

3. Bymaster FP, et al. J Pharmacol Exp Ther. 1994 Apr;269(1):282-9.

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