LY 246708 tartrate
- Product Name
- LY 246708 tartrate
- CAS No.
- 152854-19-8
- Chemical Name
- LY 246708 tartrate
- Synonyms
- Sarnomil tartrate;xanomeline tartrat;LY 246708 tartrate;Xanomeline tartrate;Zanoterone tartrate;Xanomeline L-Tartrate;(+)-L-Hydrogen 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
- CBNumber
- CB83191408
- Molecular Formula
- C18H29N3O7S
- Formula Weight
- 431.50376
- MOL File
- 152854-19-8.mol
LY 246708 tartrate Property
- 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
N-Bromosuccinimide Price
- Product number
- API0009802
- Product name
- XANOMELINE TARTRATE
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $497.66
- Updated
- 2021/12/16
LY 246708 tartrate Chemical Properties,Usage,Production
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
LY 246708 tartrate Preparation Products And Raw materials
Raw materials
Preparation Products
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