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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

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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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25 mg ￥1680 In stock
100 mg ￥4580 In stock
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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); 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; 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.

Alzheimer Disease

Phase 3 Discontinued

物理化学性质&存储条件

分子量
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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