LY 246708 tartrate CAS 152854-19-8

Introduction：Basic information about LY 246708 tartrate CAS 152854-19-8, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

LY 246708 tartrate Basic information

• Product Name: LY 246708 tartrate
• Synonyms: LY 246708 tartrate;(+)-L-Hydrogen tartrate;Xanomeline tartrate;Sarnomil tartrate;Zhan Nuo Meilin Tartrate;3-(Hexyloxy)-4-(1-methyl-1,2,5,6-tetrahydropyridin-3-yl)-1,2,5-thiadiazole (2R,3R)-2,3-dihydroxysuccinate;xanomeline tartrat;Zanoterone tartrate
• CAS: 152854-19-8
• MF: C18H29N3O7S
• MW: 431.50376
• Product Categories: API
• Mol File: 152854-19-8.mol

LY 246708 tartrate Chemical Properties

• Melting point: 95.5°
• storage temp.: -20°C
• solubility: Soluble in DMSO (45 mg/ml) or Water (70 mg/ml)
• form: solid
• color: Off-white
• Stability: Stable for 2 years from date of purchase as supplied. Solutions in DMSO or water may be stored at -20°C for up to 2 months.
• InChIKey: SJSVWTMVMBGIHQ-LREBCSMRSA-N

LY 246708 tartrate Usage And Synthesis

Description

Xanomeline tartrate (152854-19-8) functionally-selective M1 muscarinic receptor agonist, EC50=0.3, 92.5, 5, 52 and 42 nM for M1, M2, M3, M4 and M5 respectively.1,2 Displays positive cognitive and behavioral effects in schizophrenia and Alzheimer’s disease.3 Suppresses proinflammatory cytokine responses and improves survival in sepsis.4 Displays potent analgesic activity in rodent models of chronic inflammatory and neuropathic pain.5

Uses

Alzheimer’s disease treatment (cholinergic agonist).

in vivo

Xanomeline (LY 246708) (0.5-3 mg/kg; s.c.; 1-3 hours) induces salivation and vomiting in some monkeys^[3].
?Xanomeline (LY 246708) shows functional dopamine antagonism and an antipsychotic-like profile^[3].
?Xanomeline (LY 246708) inhibits D-amphetamine- and (?)-apomorphine-induced behavior and do not cause extrapyramidal side effects^[3].

• Animal Model: Male Cebus apella monkeys^[3]
• Dosage: 0.5-3 mg/kg
• Administration: s.c.; 1-3 hours
• Result: Induced salivation and vomiting in some monkeys.

References

[1] JULIA N. HEINRICH . Pharmacological comparison of muscarinic ligands: Historical versus more recent muscarinic M1-preferring receptor agonists[J]. European journal of pharmacology, 2009, 605 1: Pages 53-56. DOI:10.1016/j.ejphar.2008.12.044
[2] J JAKUBÍK. Importance and prospects for design of selective muscarinic agonists.[J]. Physiological research, 2008, 57 Suppl 3: S39-S47. DOI:10.33549/physiolres.931449
[3] AARON M. BENDER  Craig W L  Carrie K Jones. Classics in Chemical Neuroscience: Xanomeline[J]. ACS Chemical Neuroscience, 2017, 8 3: 435-443. DOI:10.1021/acschemneuro.7b00001
[4] MAURICIO ROSAS-BALLINA . Xanomeline suppresses excessive pro-inflammatory cytokine responses through neural signal-mediated pathways and improves survival in lethal inflammation[J]. Brain, Behavior, and Immunity, 2015, 44: Pages 19-27. DOI:10.1016/j.bbi.2014.07.010
[5] GIOVANNI MARTINO . The M1/M4 preferring agonist xanomeline is analgesic in rodent models of chronic inflammatory and neuropathic pain via central site of action[J]. PAIN®, 2011, 152 12: Pages 2852-2860. DOI:10.1016/j.pain.2011.09.017