Xanomeline (oxalate) (Synonyms: Lumeron, LY246708, Memcor) |
| Katalog-Nr.GC18255 |
Xanomelin (Oxalat) (LY246708-Oxalat) ist ein potenter und selektiver Muskarinrezeptor-Agonist (SMRA) und stimuliert die Phosphoinositid-Hydrolyse in vivo.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 141064-23-5
Sample solution is provided at 25 µL, 10mM.
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Xanomeline oxalate (LY246708) is a selective M1 muscarinic receptor agonist.IC50 value:Target: M1 muscarinic receptorin vitro: Xanomeline had high affinity for muscarinic receptors in brain homogenates, but had substantially less or no affinity for a number of other neurotransmitter receptors and uptake sites. In cells stably expressing genetic m1 receptors, xanomeline increased phospholipid hydrolysis in CHO, BHK and A9 L cells to 100, 72 and 55% of the nonselective agonist carbachol. In isolated tissues, xanomeline had high affinity for M1 receptors in the rabbit vas deferens (IC50 = 0.006 nM), low affinity for M2 receptors in guinea pig atria (EC50 = 3 microM), was a weak partial agonist in guinea pig ileum and was neither an agonist nor antagonist in guinea pig bladder [1]. Xanomeline produced small increases in striatal acetylcholine levels and did not antagonize the large increases in acetylcholine produced by the nonselective muscarinic agonist oxotremorine, indicating that xanomeline did not block M2 autoreceptors [2]. in vivo: Xanomeline increased striatal levels of dopamine metabolites, presumably by acting at M1 heteroreceptors on dopamine neurons to increase dopamine release. In contrast, xanomeline had only a relatively small effect on acetylcholine levels in brain, indicating that it is devoid of actions at muscarinic autoreceptors [1]. The effects of xanomeline on ex vivo binding and DOPAC levels lasted for about 3 hr and were evident after oral administration. An analog of xanomeline with similar in vivo effects did not inhibit acetylcholinesterase or choline acetyltransferase and inhibited choline uptake only at concentrations much higher than those required to inhibit binding. These data indicate xanomeline is selective agonist for M1 over M2 and M3 receptors in vivo in rat [2].
References:
[1]. Shannon HE, et al. Xanomeline: a novel muscarinic receptor agonist with functional selectivity for M1 receptors. J Pharmacol Exp Ther. 1994 Apr;269(1):271-81.
[2]. Bymaster FP, et al. Neurochemical effects of the M1 muscarinic agonist xanomeline (LY246708/NNC11-0232).J Pharmacol Exp Ther. 1994 Apr;269(1):282-9.
| Cas No. | 141064-23-5 | SDF | |
| Überlieferungen | Lumeron, LY246708, Memcor | ||
| Chemical Name | 3-[4-(hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methyl-pyridine, ethanedioate | ||
| Canonical SMILES | CCCCCCOC1=NSN=C1C2=CCCN(C)C2.OC(C(O)=O)=O | ||
| Formula | C14H23N3OS.C2H2O4 | M.Wt | 371.5 |
| Löslichkeit | DMF: 1.6 mg/ml,DMF:PBS (pH 7.2) (1:9): 0.1 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6918 mL | 13.459 mL | 26.9179 mL |
| 5 mM | 538.4 μL | 2.6918 mL | 5.3836 mL |
| 10 mM | 269.2 μL | 1.3459 mL | 2.6918 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
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