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首页-小分子抑制剂&激动剂-GPCR-mAChR-Xanomeline oxalate
Xanomeline oxalate

Chemical Structure : Xanomeline oxalate

CAS No.: 141064-23-5

Xanomeline oxalate (LY246708, LY-246708, NNC 110232)

货号: PC-43517Not For Human Use, Lab Use Only.

Xanomeline oxalate (LY246708, NNC 110232) is a potent, specific M1 muscarinic agonist with functional selectivity for M1 receptor (binding IC50 of 6 pM in the rabbit vas deferens).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Xanomeline oxalate (LY246708, NNC 110232) is a potent, specific M1 muscarinic agonist with functional selectivity for M1 receptor (binding IC50 of 6 pM in the rabbit vas deferens).
Xanomeline displays low affinity for M2 receptors in guinea pig atria (EC50=3 uM).
Xanomeline increases striatal levels of dopamine metabolites, presumably by acting at M1 heteroreceptors on dopamine neurons to increase dopamine release in vivo.
Xanomeline inhibits ex vivo binding of muscarinic radioligands to homogenates of brain and the inhibition of ex vivo binding occurred in the same dose range as increases in DOPAC levels.
Xanomeline is selective agonist for M1 over M2 and M3 receptors in vivo in rats.

物理化学性质&存储条件

分子量 371.45
分子式 C16H25N3O5S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Pyridine, 3-[4-(hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methyl-, ethanedioate (1:1)

参考文献

1. Shannon HE, et al. J Pharmacol Exp Ther. 1994 Apr;269(1):271-81.

2. Sauerberg P, et al. J Med Chem. 1992 Jun 12;35(12):2274-83.

3. Bymaster FP, et al. J Pharmacol Exp Ther. 1994 Apr;269(1):282-9.

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