CAS:886047-13-83-Amino-5-chloro-N-cyclopropyl-6-methoxy-4-methylthieno[2,3-b]pyridine-2-carboxamide

您的位置 : 首页 / Neuronal Signaling / AChR / LY 2033298 New

LY 2033298 New 3-氨基-5-氯-N-环丙基-6-甲氧基-4-甲基噻吩并[2,3-b]吡啶-2-羧酰胺 Cat No. FB16601Cas No. 886047-13-8

LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 enhances inhibition by oxotremorine of light-induced phase shifts in hamster circadian activity rhythms.

规格	价格	促销价格	库存

18817579266

立即询价

咨询

18817579266

立即询价

实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.2073 mL
- 16.0366 mL
- 32.0732 mL
- 5 mM
- 0.6415 mL
- 3.2073 mL
- 6.4146 mL
- 10 mM
- 0.3207 mL
- 1.6037 mL
- 3.2073 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号	886047-13-8	储存条件	粉末 -20°C 3 年液体 -80°C 12 月
分子式	C13H14ClN3O2S	运输	蓝冰
分子量	311.79	别名

靶点数据

生物活性

描述LY2033298 as a novel allosteric potentiator of acetylcholine (ACh) at the M(4) muscarinic acetylcholine receptor (mAChR). Radioligand-binding studies revealed that LY2033298 displayed a preference for the active state of the M(4) mAChR, manifested as a potentiation in the binding affinity of ACh (but not antagonists) and an increase in the proportion of high-affinity agonist-receptor complexes. Functional interaction studies between LY2033298 and various orthosteric and allosteric ligands revealed that its site of action overlaps with the allosteric site used by prototypical mAChR modulators. Importantly, LY2033298 reduced [(3)H]ACh release from rat striatal slices, indicating retention of its ability to allosterically potentiate endogenous ACh in situ^[1]. Mutational analysis identified a key amino acid (D(432)) in the third extracellular loop of the human M(4) receptor to be critical for selectivity and agonist potentiation by LY2033298. Importantly, LY2033298 was active in animal models predictive of clinical antipsychotic drug efficacy indicating its potential use as a first-in-class, selective, allosteric muscarinic antipsychotic agent^[2].