1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. Xanomeline oxalate

Xanomeline oxalate (Synonyms: LY246708 oxalate)

Cat. No.: HY-13410 Purity: 99.89%
Handling Instructions

Xanomeline oxalate (LY246708 oxalate) is a potent and selective muscarinic receptor agonist (SMRA) and stimulates phosphoinositide hydrolysis in vivo. Xanomeline oxalate can be used for the research of Alzheimer’s disease.

For research use only. We do not sell to patients.

Xanomeline oxalate Chemical Structure

Xanomeline oxalate Chemical Structure

CAS No. : 141064-23-5

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Solution
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 106 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 612 In-stock
Estimated Time of Arrival: December 31
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Description

Xanomeline oxalate (LY246708 oxalate) is a potent and selective muscarinic receptor agonist (SMRA) and stimulates phosphoinositide hydrolysis in vivo. Xanomeline oxalate can be used for the research of Alzheimer’s disease[1].

IC50 & Target

muscarinic receptor[1]

In Vitro

Xanomeline stimulates phosphoinositide (PI) hydrolysis in the A9 L m1 cells[1].
Xanomeline inhibits [3H]-pirenzepine ([3H]-PZ) and [3H]-oxotremorine-M ([3H]-OXO-M) binding to rat brain with Kis of 7 and 3 nM, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Xanomeline robustly stimulates in vivo PI hydrolysis and the effect is blocked by muscarinic antagonists, demonstrating mediation by muscarinic receptors. In mice the ED100 for Xanomeline-induced stimulation of [3H]-IP accumulation is 54 μmole/kg in hippocampus. And in rats the ED100 for Xanomeline-induced stimulation of [3H]-IP accumulation is 8.1 μmole/kg in hippocampus[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male CF1 mice weighing 18-20 g are injected [3H]-myoinositol[1]
Dosage: 8.1-81 μmole/kg
Administration: S.c. injections; 1 h prior to killing and 1 h after the administration
Result: Increased accumulation in a dose-related manner up to 130%, 75%, 60% above lithium levels in hippocampus, cortex and neostriatum, respectively. And did not increase accumulation of [3H]-IP in the brain stem. Induced salivation, tremor and hypothermia in mice with the ED50 of 13.7±0.8 μmole/kg.
Animal Model: Rats are injected [3H]-myoinositol[1]
Dosage: 2.7-81 μmole/kg
Administration: S.c. injections; 1 h prior to killing and 1 h after the administration
Result: Increased [3H]-IP formation dose dependently in hippocampus up to 221% above lithium control.
Clinical Trial
Molecular Weight

371.45

Formula

C16H25N3O5S

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (134.61 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6922 mL 13.4608 mL 26.9215 mL
5 mM 0.5384 mL 2.6922 mL 5.3843 mL
10 mM 0.2692 mL 1.3461 mL 2.6922 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

*All of the co-solvents are available by MCE.
References

Purity: 99.89%

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Product Name:
Xanomeline oxalate
Cat. No.:
HY-13410
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