| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Xanomeline oxalate (also known as LY246708) is a novel, potent and selective M1 muscarinic receptor agonist with good selectivity for the M1 and M4 subtypes. It has been researched for treating negative and cognitive symptoms of schizophrenia as well as Alzheimer's disease, though gastrointestinal side effects caused a high clinical trial dropout rate. In spite of this, xanomeline has been demonstrated to be reasonably effective in treating the symptoms of schizophrenia. A recent study conducted on humans revealed that xanomeline treatment was associated with significant improvements in verbal learning and short-term memory.
| Targets |
muscarinic receptor
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|---|---|
| ln Vitro |
Xanomeline oxalate stimulates phosphoinositide (PI) potential in A9 L m1 cells [1]. M) binds to the brain with Ki of 7 and 3 nM respectively[1].
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| ln Vivo |
Xanomeline oxalate strongly stimulates PI responses in vivo, and this effect is boiled by muscarinic-selective antioxidants, suggesting that it is mediated by muscarinic receptors. In mice, the ED100 of [3H]-IP accumulation in the hippocampus induced by Xanomeline oxalate was 54 μMole/kg. In the trajectory, the ED100 of [3H]-IP accumulation in the hippocampus induced by Xanomeline oxalate was 8.1 μMole/kg[1]. Animal model: Male CF1 mice weighing 18-20 g were injected with [3H]-inositol[1]. Dosage: 8.1-81 μmole/kg. Administration method: subcutaneous injection; 1 hour before sacrifice and 1 hour after administration. Results: Lithium levels increased in a dose-related manner in the hippocampus, cortex, and neostriatum, up to 130%, 75%, and 60%, respectively. and does not increase the accumulation of [3H]-IP in the brainstem. Induces salivation, tremors and hypothermia in mice with an ED50 of 13.7±0.8 μmole/kg. Animal model: Rats were injected with [3H]-inositol[1]. Dosage: 2.7-81 μmole/kg. Administration method: subcutaneous injection; 1 hour before sacrifice and 1 hour after administration. Results: [3H]-IP formation in hippocampus. Dose-dependent increase, 221% higher than lithium control.
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| Animal Protocol |
Male CF1 mice weighing 18-20 g are injected [3H]-myoinositol
8.1-81 μmole/kg S.c. injections; 1 h prior to killing and 1 h after the administration |
| References |
| Molecular Formula |
C16H25N3O5S
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|---|---|
| Molecular Weight |
371.4518
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| Exact Mass |
281.16
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| Elemental Analysis |
C, 51.74; H, 6.78; N, 11.31; O, 21.54; S, 8.63
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| CAS # |
141064-23-5
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| Related CAS # |
Xanomeline; 131986-45-3
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| Appearance |
White to off-white solid powder
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| SMILES |
CCCCCCOC1=NSN=C1C2=CCCN(C2)C.C(=O)(C(=O)O)O
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| InChi Key |
ZJOUESNWCLASJP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H23N3OS.C2H2O4/c1-3-4-5-6-10-18-14-13(15-19-16-14)12-8-7-9-17(2)11-12;3-1(4)2(5)6/h8H,3-7,9-11H2,1-2H3;(H,3,4)(H,5,6)hI=1S/C14H23N3OS.C2H2O4/c1-3-4-5-6-10-18-14-13(15-19-16-14)12-8-7-9-17(2)11-12;3-1(4)2(5)6/h8H,3-7,9-11H2,1-2H3;(H,3,4)(H,5,6)
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| Chemical Name |
3-hexoxy-4-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazole;oxalic acid
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| Synonyms |
LY-246708; LY246708; LY 246708; Memcor; NNC-110232; Hexyloxy-TZTP; HexyloxyTZTP
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~134.6 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.73 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 (6.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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 (6.73 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 | 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 |
*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.
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