Size | Price | Stock | Qty |
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5mg |
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10mg |
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50mg |
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100mg |
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Other Sizes |
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Targets |
mAChR1 mAChR4
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ln Vitro |
The mean firing rate increased overall in response to xanomeline (0.1~10 μM; CNS4U). The functionality of M1 receptors in neurons produced from hiPSCs is demonstrated by xanomeline. When xanomeline (>1 μM) attaches to receptors, it activates them for an extended amount of time, which keeps the M current from flowing [1].
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ln Vivo |
In certain monkeys, xanomeline (0.5~3 mg/kg; sc; 1~3 hours) induces vomiting and salivation[3]. Xanomeline exhibits properties resembling those of an antipsychotic and functional dopamine antagonist. Xanomeline prevents extrapyramidal side effects while blocking behaviors brought on by D-amphetamine and ()-apomorphine[3].
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Animal Protocol |
Animal/Disease Models: Male Cebus apella monkeys
Doses: 0.5~3 mg/kg Route of Administration: Sc; 1~3 hrs (hours) Experimental Results: Induced salivation and vomiting in some monkeys. |
References |
[1]. Kreir M, et al. Role of Kv7.2/Kv7.3 and M1 muscarinic receptors in the regulation of neuronal excitability in hiPSC-derived neurons. Eur J Pharmacol. 2019;858:172474
[2]. Shekhar A, et al. Selective muscarinic receptor agonist xanomeline as a novel treatment approach for schizophrenia. Am J Psychiatry. 2008;165(8):1033-1039. [3]. Andersen MB, et al. The muscarinic M1/M4 receptor agonist xanomeline exhibits antipsychotic-like activity in Cebus apella monkeys. Neuropsychopharmacology. 2003;28(6):1168-1175. |
Molecular Formula |
C14H23N3OS
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Molecular Weight |
281.42
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CAS # |
131986-45-3
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Related CAS # |
Xanomeline tartrate;152854-19-8;Xanomeline oxalate;141064-23-5
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
S1N=C(C(C2=C([H])C([H])([H])C([H])([H])N(C([H])([H])[H])C2([H])[H])=N1)OC([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H]
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: 50 mg/mL (177.67 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.88 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (8.88 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.5534 mL | 17.7670 mL | 35.5341 mL | |
5 mM | 0.7107 mL | 3.5534 mL | 7.1068 mL | |
10 mM | 0.3553 mL | 1.7767 mL | 3.5534 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.